-
2
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-
85030303914
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Recombinant Capital Database on World Wide Web URL:
-
Recombinant Capital Database on World Wide Web URL: http://www.recap.com.
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-
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3
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0031116628
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Combinatorial chemistry and new drugs
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of outstanding interest. A review of the different approaches to combinatorial chemistry and, in particular, some reports of drug discovery using the technology.
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Plunkett MJ, Ellman JA. Combinatorial chemistry and new drugs. of outstanding interest Sci Am. 276:1997;69-73 A review of the different approaches to combinatorial chemistry and, in particular, some reports of drug discovery using the technology.
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Sci Am
, vol.276
, pp. 69-73
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Plunkett, M.J.1
Ellman, J.A.2
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4
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2842561522
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Design, synthesis and evaluation of small molecule libraries
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of outstanding interest. A comprehensive review of chemical synthesis approaches to small molecule libraries.
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Ellman JA. Design, synthesis and evaluation of small molecule libraries. of outstanding interest Acc Chem Res. 29:1996;132-143 A comprehensive review of chemical synthesis approaches to small molecule libraries.
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(1996)
Acc Chem Res
, vol.29
, pp. 132-143
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Ellman, J.A.1
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5
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0000108684
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The synthesis of a 1680 mmeber 1,4-benzodiazepine library
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of outstanding interest. Synthesis of a 1,4-benzodiazepine library on solid support from readily available building blocks.
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Bunin BA, Plunkett MJ, Ellman JA. The synthesis of a 1680 mmeber 1,4-benzodiazepine library. of outstanding interest New J Chem. 21:1997;125-130 Synthesis of a 1,4-benzodiazepine library on solid support from readily available building blocks.
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New J Chem
, vol.21
, pp. 125-130
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Bunin, B.A.1
Plunkett, M.J.2
Ellman, J.A.3
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6
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0030932342
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Solid-phase synthesis of 1,4-benzodiazepine-2,5-diones. Library preparation and demonstration of synthesis generality
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of special interest. An extension of benzodiazepine motif libraries; the synthesis of novel 1,4-benzodiazepine-2,5-diones as potentially active compounds.
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Boojamra CG, Burow KM, Thomson LA, Ellman JA. Solid-phase synthesis of 1,4-benzodiazepine-2,5-diones. Library preparation and demonstration of synthesis generality. of special interest J Org Chem. 62:1997;1240-1256 An extension of benzodiazepine motif libraries; the synthesis of novel 1,4-benzodiazepine-2,5-diones as potentially active compounds.
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(1997)
J Org Chem
, vol.62
, pp. 1240-1256
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Boojamra, C.G.1
Burow, K.M.2
Thomson, L.A.3
Ellman, J.A.4
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7
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0030443529
-
A remarkable two-step synthesis of diverse 1,4-benzodiazepine-2,5-diones using the Ugi four-component condensation
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of outstanding interest. An alternative and remarkably concise two-step synthesis of 1,4-benzo diazepine-2,5-diones.
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Keating TA, Armstrong RW. A remarkable two-step synthesis of diverse 1,4-benzodiazepine-2,5-diones using the Ugi four-component condensation. of outstanding interest J Org Chem. 61:1996;8935-8939 An alternative and remarkably concise two-step synthesis of 1,4-benzo diazepine-2,5-diones.
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(1996)
J Org Chem
, vol.61
, pp. 8935-8939
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Keating, T.A.1
Armstrong, R.W.2
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8
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0030034999
-
Solid phase synthesis of hydantoins using a carbonate linker and a novel cyclization/cleavage step
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Dressman BA, Spangle LA, Kaldor SW. Solid phase synthesis of hydantoins using a carbonate linker and a novel cyclization/cleavage step. Tetrahedron Lett. 37:1996;937-940.
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(1996)
Tetrahedron Lett
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, pp. 937-940
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Dressman, B.A.1
Spangle, L.A.2
Kaldor, S.W.3
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9
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0030976794
-
Solid phase synthesis of hydantoin library using a novel cyclization and traceless cleavage step
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Kim SW, Ahn SY, Koh JS, Lee JH, Ro S, Cho HY. Solid phase synthesis of hydantoin library using a novel cyclization and traceless cleavage step. Tetrahedron Lett. 38:1997;4603-4606.
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(1997)
Tetrahedron Lett
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Kim, S.W.1
Ahn, S.Y.2
Koh, J.S.3
Lee, J.H.4
Ro, S.5
Cho, H.Y.6
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11
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0031575637
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Combinatorial synthesis of 2,9-substituted purines
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Gray NS, Kwon S, Schultz PG. Combinatorial synthesis of 2,9-substituted purines. Tetrahedron Lett. 38:1997;1161-1164.
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Tetrahedron Lett
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Gray, N.S.1
Kwon, S.2
Schultz, P.G.3
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12
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0031152054
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Combinatorial approaches to carbohydrates
-
of outstanding interest. Rapid construction of oligosaccharides by forming multiple glycosidic linkages in a single step. The synthetic sequence takes advantage of the fact that the relative reactivity of glycosidic residues containing anomeric sulfoxides and nucleophilic functional groups can be controlled. Sequence can be extended to synthesis on a solid support.
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Kahne DE. Combinatorial approaches to carbohydrates. of outstanding interest Curr Opin Chem Biol. 1:1997;130-135 Rapid construction of oligosaccharides by forming multiple glycosidic linkages in a single step. The synthetic sequence takes advantage of the fact that the relative reactivity of glycosidic residues containing anomeric sulfoxides and nucleophilic functional groups can be controlled. Sequence can be extended to synthesis on a solid support.
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(1997)
Curr Opin Chem Biol
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, pp. 130-135
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Kahne, D.E.1
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13
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0029996782
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A new method for the solid phase synthesis of oligosaccharides
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Rademann J, Schmidt RR. A new method for the solid phase synthesis of oligosaccharides. Tetrahedron Lett. 37:1996;3989-3990.
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Tetrahedron Lett
, vol.37
, pp. 3989-3990
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Rademann, J.1
Schmidt, R.R.2
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14
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0030575428
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Solid phase synthesis of oligosaccharides
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Adinolfi M, Barone G, DeNapoli L, Iadonisi A, Piccialli G. Solid phase synthesis of oligosaccharides. Tetrahedron Lett. 37:1996;5007-5010.
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Tetrahedron Lett
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Adinolfi, M.1
Barone, G.2
Denapoli, L.3
Iadonisi, A.4
Piccialli, G.5
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15
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0030605136
-
A method for the synthesis of hydroxamic acids on solid phase
-
of special interest. A library synthesis of hydroxamic acids on a Wang resin. The compounds are potential inhibitors of matrix metalloproteinases.
-
Floyd CD, Lewis CN, Patel SR, Whittaker M. A method for the synthesis of hydroxamic acids on solid phase. of special interest Tetrahedron Lett. 37:1996;8045-8048 A library synthesis of hydroxamic acids on a Wang resin. The compounds are potential inhibitors of matrix metalloproteinases.
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(1996)
Tetrahedron Lett
, vol.37
, pp. 8045-8048
-
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Floyd, C.D.1
Lewis, C.N.2
Patel, S.R.3
Whittaker, M.4
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17
-
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0031550887
-
Solid phase synthesis of peptide hydroxamic acids
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of special interest. Solid phase synthesis of a peptide hydroxamic acid library.
-
Chen JJ, Spatola AF. Solid phase synthesis of peptide hydroxamic acids. of special interest Tetrahedron Lett. 38:1997;1511-1514 Solid phase synthesis of a peptide hydroxamic acid library.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 1511-1514
-
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Chen, J.J.1
Spatola, A.F.2
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18
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0031127997
-
Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D
-
of outstanding interest. A combined approach of rational structure-based design and combinatorial chemsitry to identify potent inhibitors of Cathepsin D, an aspartyl protease.
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Kick EK, Roe DC, Skillman AG, Lin G, Ewing TJA, Sun Y, Kuntz ID, Ellman JA. Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D. of outstanding interest Chem Biol. 4:1997;297-307 A combined approach of rational structure-based design and combinatorial chemsitry to identify potent inhibitors of Cathepsin D, an aspartyl protease.
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(1997)
Chem Biol
, vol.4
, pp. 297-307
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Kick, E.K.1
Roe, D.C.2
Skillman, A.G.3
Lin, G.4
Ewing, T.J.A.5
Sun, Y.6
Kuntz, I.D.7
Ellman, J.A.8
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19
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0031031681
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Development of the new potent non-peptide Gp IIb/IIIa antagonist NSL-95301 by using combinatorial technique
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Harada T, Katada J, Tachiki A, Asari T, Iijima K, Uno I, Ojima I, Hayashi Y. Development of the new potent non-peptide Gp IIb/IIIa antagonist NSL-95301 by using combinatorial technique. Biorg Med Chem Lett. 7:1997;209-212.
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Biorg Med Chem Lett
, vol.7
, pp. 209-212
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Harada, T.1
Katada, J.2
Tachiki, A.3
Asari, T.4
Iijima, K.5
Uno, I.6
Ojima, I.7
Hayashi, Y.8
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21
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10544220839
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Selection of potent inhibitors of farnesyl-protein transferase from a synthetic tetrapeptide combinatorial library
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Wallace A, Koblan KS, Hamilton K, Marquis-Omer DJ, Miller PJ, Mosser SD, Omer CA, Schaber MD, Cortese R, Oliff A, et al. Selection of potent inhibitors of farnesyl-protein transferase from a synthetic tetrapeptide combinatorial library. J Biol Chem. 271:1996;31306-31311.
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J Biol Chem
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, pp. 31306-31311
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Wallace, A.1
Koblan, K.S.2
Hamilton, K.3
Marquis-Omer, D.J.4
Miller, P.J.5
Mosser, S.D.6
Omer, C.A.7
Schaber, M.D.8
Cortese, R.9
Oliff, A.10
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23
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0029783934
-
Neighborhood behaviour: A useful concept for validation of molecular diversity descriptors
-
of outstanding interest. The two facets of drug discovery, notably lead generation and lead optimization, are discussed in relationship to the particular molecular diversity descriptors that need to be employed. A concept of identifying an activity island (by lead generation) followed by detailed exploration of the island (lead optimization) is used as the basis of examining the validity of different descriptors.
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Patterson DE, Cramer RD, Ferguson AM, Clark RD, Weinberger LE. Neighborhood behaviour: a useful concept for validation of molecular diversity descriptors. of outstanding interest J Med Chem. 39:1996;3049-3059 The two facets of drug discovery, notably lead generation and lead optimization, are discussed in relationship to the particular molecular diversity descriptors that need to be employed. A concept of identifying an activity island (by lead generation) followed by detailed exploration of the island (lead optimization) is used as the basis of examining the validity of different descriptors.
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(1996)
J Med Chem
, vol.39
, pp. 3049-3059
-
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Patterson, D.E.1
Cramer, R.D.2
Ferguson, A.M.3
Clark, R.D.4
Weinberger, L.E.5
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24
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0002656809
-
Designing chemical libraries for lead discovery
-
of outstanding interest. The authors focus on so-called Optiverse™ libraries which are designed to identify initial hits against any biological target. The library molecules are deliberately designed to be dissimilar from one another based upon specific 2D-diversity fingerprints.
-
Ferguson AM, Patterson DE, Gary CD, Underiner TL. Designing chemical libraries for lead discovery. of outstanding interest J Biomol Screening. 1:1996;65-73 The authors focus on so-called Optiverse™ libraries which are designed to identify initial hits against any biological target. The library molecules are deliberately designed to be dissimilar from one another based upon specific 2D-diversity fingerprints.
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(1996)
J Biomol Screening
, vol.1
, pp. 65-73
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Ferguson, A.M.1
Patterson, D.E.2
Gary, C.D.3
Underiner, T.L.4
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25
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0003230848
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Novel software tools for addressing chemical diversity
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set of molecules which can best represent the full range of chemical diversity present in the really large libraries of special interest
-
Pearlman RS. Novel software tools for addressing chemical diversity. of special interest Network Science. 1996; The author discusses software tools for addressing chemical diversity to identify a small library sub-set of molecules which can best represent the full range of chemical diversity present in the really large libraries.
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(1996)
Network Science
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Pearlman, R.S.1
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26
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0005757079
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Combinatorial chemistry library design using pharmacophore diversity
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The use of pharmacophore hypotheses to quantify diversity of molecules within a library are discussed. Emphasis is given to the 3D conformations of the molecules rather than simple topological approaches as discussed by Ferguson et al. 1996 [24] of special interest. of outstanding interest
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of special interest Davies K, Briant C. Combinatorial chemistry library design using pharmacophore diversity. of outstanding interest Network Science. 1996; The use of pharmacophore hypotheses to quantify diversity of molecules within a library are discussed. Emphasis is given to the 3D conformations of the molecules rather than simple topological approaches as discussed by Ferguson et al. 1996 [24].
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(1996)
Network Science
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Davies, K.1
Briant, C.2
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27
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0031152087
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Computational approaches for combinatorial library design and molecular diversity analysis
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of outstanding interest. The authors review different approaches which have been taken to identify and validate the various descriptors employed to quantify molecular diversity.
-
Blaney JM, Martin EJ. Computational approaches for combinatorial library design and molecular diversity analysis. of outstanding interest Curr Opin Chem Biol. 1:1997;54-59 The authors review different approaches which have been taken to identify and validate the various descriptors employed to quantify molecular diversity.
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(1997)
Curr Opin Chem Biol
, vol.1
, pp. 54-59
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Blaney, J.M.1
Martin, E.J.2
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28
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0000465937
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Diversity profiling and design using 3D pharmacophores: Pharmacophore-derived queries (PDQ)
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of outstanding interest. Mason et al. describe the use of a 3D (3-point) pharmacophore approach to measuring diversity. Results from profiling a large corporate database and examples of combinatorial libraries are discussed and contrasted with an alternative approach utilizing commercially available software.
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Pickett SD, Mason JS, McLay IM. Diversity profiling and design using 3D pharmacophores: pharmacophore-derived queries (PDQ). of outstanding interest J Chem Int Comput Sci. 36:1996;1214-1223 Mason et al. describe the use of a 3D (3-point) pharmacophore approach to measuring diversity. Results from profiling a large corporate database and examples of combinatorial libraries are discussed and contrasted with an alternative approach utilizing commercially available software.
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(1996)
J Chem Int Comput Sci
, vol.36
, pp. 1214-1223
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Pickett, S.D.1
Mason, J.S.2
McLay, I.M.3
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29
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0030943408
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Selecting optimally diverse compounds from structure databases: A validation study of two-dimensional and three-dimensional descriptors
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of special interest. The use of 2D and 3D molecular descriptors are contrasted in the two phases of drug discovery (lead generation and optimization).
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Matter H. Selecting optimally diverse compounds from structure databases: a validation study of two-dimensional and three-dimensional descriptors. of special interest J Med Chem. 40:1997;1219-1229 The use of 2D and 3D molecular descriptors are contrasted in the two phases of drug discovery (lead generation and optimization).
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(1997)
J Med Chem
, vol.40
, pp. 1219-1229
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Matter, H.1
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30
-
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0002583384
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Rapid reliable drug discovery
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of outstanding interest. A unique approach to library design explores the concept of molecules which are promiscuous in behavior rather than diverse. Such molecules are deliberately selected to have the capability to potentially interact with a wide range of targets and this allows libraries containing them to be much smaller in size. An iterative cycle decodes the relevant molecules with the appropriate recognition features for a specific target.
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Myers PL, Greene JW, Saunders J, Teig SL. Rapid reliable drug discovery. of outstanding interest Todays Chemist at Work. 6:1997;47-53 A unique approach to library design explores the concept of molecules which are promiscuous in behavior rather than diverse. Such molecules are deliberately selected to have the capability to potentially interact with a wide range of targets and this allows libraries containing them to be much smaller in size. An iterative cycle decodes the relevant molecules with the appropriate recognition features for a specific target.
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(1997)
Todays Chemist at Work
, vol.6
, pp. 47-53
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Myers, P.L.1
Greene, J.W.2
Saunders, J.3
Teig, S.L.4
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31
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0030815955
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Designing combinatorial library mixtures using a genetic algorithm
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of special interest. The use of a genetic algorithm is discussed which enables the optimal trade-off in overall diversity coupled with efficient deconvolution in library design.
-
Brown RD, Martin YC. Designing combinatorial library mixtures using a genetic algorithm. of special interest J Med Chem. 40:1997;2304-2313 The use of a genetic algorithm is discussed which enables the optimal trade-off in overall diversity coupled with efficient deconvolution in library design.
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(1997)
J Med Chem
, vol.40
, pp. 2304-2313
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Brown, R.D.1
Martin, Y.C.2
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33749842822
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Optimization of the biological activity of combinatorial compound libraries by a genetic algorithm
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Int Ed Engl
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Weber L, Wallbaum S, Broger C, Gubernator K. Optimization of the biological activity of combinatorial compound libraries by a genetic algorithm. Int Ed Engl Angew Chem. 34:1995;2281-2282.
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Angew Chem
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Weber, L.1
Wallbaum, S.2
Broger, C.3
Gubernator, K.4
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33
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85030301796
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Molecumetics on World Wide Site URL: of special interest
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Molecumetics on World Wide Site URL: http/www.molecumetics.com/indexcov.htm of special interest.
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34
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85030304440
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Smart libraries were used to identify a series of novel thrombin inhibitors.
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Smart libraries were used to identify a series of novel thrombin inhibitors.
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35
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0031569368
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Serendipity meets precision: The integration of structure-based drug design and combinatorial chemistry for efficient drug discovery
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of special interest. Structure-based design approaches linked to automated synthesis has given active thrombin inhibitors.
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Salemme FR, Spurlino J, Bone R. Serendipity meets precision: the integration of structure-based drug design and combinatorial chemistry for efficient drug discovery. of special interest Curr Biol. 5:1997;319-324 Structure-based design approaches linked to automated synthesis has given active thrombin inhibitors.
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(1997)
Curr Biol
, vol.5
, pp. 319-324
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Salemme, F.R.1
Spurlino, J.2
Bone, R.3
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36
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0343593774
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An automated analytical/preparative LC/MS system for the characterization and purification of compound libraries
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of outstanding interest
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Zeng L, Burton L, Yung K, Shushan B, Kassel DB. An automated analytical/preparative LC/MS system for the characterization and purification of compound libraries. of outstanding interest J Chromatogr A. 1997; The authors review the development of automated liquid chromatography/mass spectroscopy as a tool for both rapid analysis and final purification of library compounds.
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(1997)
J Chromatogr a
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Zeng, L.1
Burton, L.2
Yung, K.3
Shushan, B.4
Kassel, D.B.5
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33748237769
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Organic synthesis on solid supports
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Fruchtel JS, Jung G. Organic synthesis on solid supports. Int Ed Angew Chem. 35:1996;17-42.
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Angew Chem
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Fruchtel, J.S.1
Jung, G.2
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38
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7044263277
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Synthesis and applications of small molecule libraries
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of special interest. A comprehensive review containing may examples of small library synthesis. Examples of active drug structures are highlighted. See also Choong et al. 1996 [38].
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Thompson LA, Ellman JA. Synthesis and applications of small molecule libraries. of special interest Chem Rev. 96:1996;555-600 A comprehensive review containing may examples of small library synthesis. Examples of active drug structures are highlighted. See also Choong et al. 1996 [38].
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Chem Rev
, vol.96
, pp. 555-600
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Thompson, L.A.1
Ellman, J.A.2
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77956743376
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Choong IC, Ellman JA. Solid phase synthesis applications to combinatorial libraries. Annu Rep Med Chem. 31:1996;309-318.
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Annu Rep Med Chem
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Choong, I.C.1
Ellman, J.A.2
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41
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7444256652
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The current status of heterocyclic combinatorial libraries
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of special interest. The current status of heterocyclic combinatorial libraries is reviewed in this publication.
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Nefzi A, Ostresh JM, Houghten RA. The current status of heterocyclic combinatorial libraries. of special interest Chem Rev. 97:1997;449-472 The current status of heterocyclic combinatorial libraries is reviewed in this publication.
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Chem Rev
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Nefzi, A.1
Ostresh, J.M.2
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J.A. Bristol.
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Bristol JA. Applications in solid-supported organic synthesis in combinatorial chemistry. Tetrahedron. 53:1997;6573-6706.
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Tetrahedron
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43
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0030987008
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Solid phase synthesis of fused bicyclic amino acid derivatives via intramolecular Pauson-Khand cyclization: Versatile scaffolds for combinatorial chemistry
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of outstanding interest. The Pauson-Khand reaction has been modified for solid phase synthesis to yield a library of complex bicyclic amino acid scaffolds capable of further functionalization.
-
Bolton GL, Hodges JC, Rubin JR. Solid phase synthesis of fused bicyclic amino acid derivatives via intramolecular Pauson-Khand cyclization: versatile scaffolds for combinatorial chemistry. of outstanding interest Tetrahedron. 53:1997;6611-6634 The Pauson-Khand reaction has been modified for solid phase synthesis to yield a library of complex bicyclic amino acid scaffolds capable of further functionalization.
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(1997)
Tetrahedron
, vol.53
, pp. 6611-6634
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Bolton, G.L.1
Hodges, J.C.2
Rubin, J.R.3
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44
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0031592570
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Solid-phase synthesis of indoles using the palladium-catalysed coupling of alkynes with iodoamine derivatives
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Fagnola MC, Candiani I, Visentin G, Cabri W, Zarini F, Mongelli N, Bedeschi A. Solid-phase synthesis of indoles using the palladium-catalysed coupling of alkynes with iodoamine derivatives. Tetrahedron Lett. 38:1997;2307-2310.
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Tetrahedron Lett
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Fagnola, M.C.1
Candiani, I.2
Visentin, G.3
Cabri, W.4
Zarini, F.5
Mongelli, N.6
Bedeschi, A.7
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45
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0031592575
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Solid-phase synthesis of 2-substituted benzofurans via the palladium-catalysed heteroannulation of acetylenes
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Fancelli D, Fagnola MC, Severino D, Bedeschi A. Solid-phase synthesis of 2-substituted benzofurans via the palladium-catalysed heteroannulation of acetylenes. Tetrahedron Lett. 38:1997;2311-2314.
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Tetrahedron Lett
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Fancelli, D.1
Fagnola, M.C.2
Severino, D.3
Bedeschi, A.4
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46
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33748225668
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Stereoselective solid-phase synthesis of cyclopentane and cyclohexane derivatives by two-component domino reactions: Generation of combinatorial libraries
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Int Ed
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Tietze LF, Steinmetz A. Stereoselective solid-phase synthesis of cyclopentane and cyclohexane derivatives by two-component domino reactions: generation of combinatorial libraries. Int Ed Angew Chem. 35:1996;651-652.
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Angew Chem
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Tietze, L.F.1
Steinmetz, A.2
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48
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0030939020
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Exploitation of the Ugi 4CC reaction: Preparation of small molecule combinatorial libraries via solid phase
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of special interest. This publication, along with Armstrong et al. 1996 [48], describes the exploitation of multicomponent reactions in library synthesis. The Ugi reaction is highlighted specifically, but other potential multiple component condensations are reviewed.
-
Short KM, Ching BW, Mjalli AMM. Exploitation of the Ugi 4CC reaction: preparation of small molecule combinatorial libraries via solid phase. of special interest Tetrahedron. 53:1997;6653-6679 This publication, along with Armstrong et al. 1996 [48], describes the exploitation of multicomponent reactions in library synthesis. The Ugi reaction is highlighted specifically, but other potential multiple component condensations are reviewed.
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(1997)
Tetrahedron
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, pp. 6653-6679
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Short, K.M.1
Ching, B.W.2
Mjalli, A.M.M.3
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Multiple-component condensation strategies for combinatorial library synthesis
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Armstrong RW, Combs AP, Tempest PA, Brown SD, Keating TA. Multiple-component condensation strategies for combinatorial library synthesis. Acc Chem Res. 29:1996;123-131.
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Acc Chem Res
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Armstrong, R.W.1
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Brown, S.D.4
Keating, T.A.5
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50
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0013613657
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A silicon-based linker for traceless solid-phase synthesis. Photodetachable arylsilane polymer linkages for use in solid phase organic synthesis
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Showalter HDH. A silicon-based linker for traceless solid-phase synthesis. Photodetachable arylsilane polymer linkages for use in solid phase organic synthesis. ChemTracts Org Chem. 9:1996;231-236.
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ChemTracts Org Chem
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, pp. 231-236
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Showalter, H.D.H.1
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51
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0000576958
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Development of a novel silyl ether linker for a solid-phase organic synthesis
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Showalter HDH, Boehm TL. Development of a novel silyl ether linker for a solid-phase organic synthesis. J Org Chem. 61:1996;6498-6499.
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(1996)
J Org Chem
, vol.61
, pp. 6498-6499
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Showalter, H.D.H.1
Boehm, T.L.2
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52
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0031032613
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Traceless linker: Oxidative activation and displacement of a sulfur-based linker
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Gayo LM, Suto MJ. Traceless linker: oxidative activation and displacement of a sulfur-based linker. Tetrahedron Lett. 38:1997;211-214.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 211-214
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Gayo, L.M.1
Suto, M.J.2
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53
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0030583495
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Application of polymer-bound phosphonium salts as traceless supports for solid phase synthesis
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Hughes I. Application of polymer-bound phosphonium salts as traceless supports for solid phase synthesis. Tetrahedron Lett. 37:1996;7595-7598.
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(1996)
Tetrahedron Lett
, vol.37
, pp. 7595-7598
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Hughes, I.1
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54
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0030458313
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Reissert-based traceless solid-phase synthesis: Isoquinoline and isoxazoline-containing heterocycles
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Lorsbach BA, Miller RB, Kurth MJ. Reissert-based traceless solid-phase synthesis: isoquinoline and isoxazoline-containing heterocycles. J Org Chem. 61:1996;8716-8717.
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(1996)
J Org Chem
, vol.61
, pp. 8716-8717
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Lorsbach, B.A.1
Miller, R.B.2
Kurth, M.J.3
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55
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0031151959
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Encoding methods for combinatorial chemistry
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Czarnik AW. Encoding methods for combinatorial chemistry. Curr Opin Chem Biol. 1:1997;60-66.
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(1997)
Curr Opin Chem Biol
, vol.1
, pp. 60-66
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Czarnik, A.W.1
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56
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0029039490
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Structure determination in combinatorial chemistry: Utilization of magic angle spinning HQMC and TOCSY NMR spectra in the structure determination of Wang-bound lysine
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Anderson RC, Stokes JP, Sharpio MJ. Structure determination in combinatorial chemistry: utilization of magic angle spinning HQMC and TOCSY NMR spectra in the structure determination of Wang-bound lysine. Tetrahedron Lett. 36:1995;5311-5314.
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(1995)
Tetrahedron Lett
, vol.36
, pp. 5311-5314
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Anderson, R.C.1
Stokes, J.P.2
Sharpio, M.J.3
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57
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0002108435
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A comparison of NMR spectra obtained for solid-phase-synthesis resins using conventional high-resolution, magic-angle-spinning and high-resolution magic-angle-spinning probes
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Keifer PA, Baltusis L, Rice DM, Tymiak AA, Shoolery JN. A comparison of NMR spectra obtained for solid-phase-synthesis resins using conventional high-resolution, magic-angle-spinning and high-resolution magic-angle-spinning probes. J Mag Res, Ser A. 119:1996;65-75.
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(1996)
J Mag Res, Ser a
, vol.119
, pp. 65-75
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Keifer, P.A.1
Baltusis, L.2
Rice, D.M.3
Tymiak, A.A.4
Shoolery, J.N.5
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58
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0030200010
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Magic angle spinning NMR: A valuable tool for monitoring the progress of reaction in solid phase synthesis
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Wehler T, Westman J. Magic angle spinning NMR: a valuable tool for monitoring the progress of reaction in solid phase synthesis. Tetrahedron Lett. 37:1996;4771-4774.
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(1996)
Tetrahedron Lett
, vol.37
, pp. 4771-4774
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Wehler, T.1
Westman, J.2
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59
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0029871215
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An NMR method to identify nondestructively chemical compounds bound to a single solid-phase-synthesis bead for combinatorial chemistry applications
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Sarkar SK, Garigipati RS, Adams JL, Keifer PA. An NMR method to identify nondestructively chemical compounds bound to a single solid-phase-synthesis bead for combinatorial chemistry applications. J Am Chem Soc. 118:1996;2305-2306.
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(1996)
J Am Chem Soc
, vol.118
, pp. 2305-2306
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Sarkar, S.K.1
Garigipati, R.S.2
Adams, J.L.3
Keifer, P.A.4
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60
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0030576861
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Monitoring of a three-step solid phase synthesis involving a Heck reaction using magic angle spinning NMR spectroscopy
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of special interest. In this paper, the use of magic angle spinning NMR is exemplified as a tool for following step-by-step reaction progress on a solid support.
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Pop IE, Dhalluin CF, Deprez BP, Melnyk PC, Lippens GM, Tartar AL. Monitoring of a three-step solid phase synthesis involving a Heck reaction using magic angle spinning NMR spectroscopy. of special interest Tetrahedron. 52:1996;12209-12222 In this paper, the use of magic angle spinning NMR is exemplified as a tool for following step-by-step reaction progress on a solid support.
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(1996)
Tetrahedron
, vol.52
, pp. 12209-12222
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Pop, I.E.1
Dhalluin, C.F.2
Deprez, B.P.3
Melnyk, P.C.4
Lippens, G.M.5
Tartar, A.L.6
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61
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0030580342
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An indazole synthesis on solid support monitored by single bead FTIR microspectroscopy
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Yan B, Gstach H. An indazole synthesis on solid support monitored by single bead FTIR microspectroscopy. Tetrahedron Lett. 37:1996;8325-8328.
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(1996)
Tetrahedron Lett
, vol.37
, pp. 8325-8328
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Yan, B.1
Gstach, H.2
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62
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0030364066
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Tools for combinatorial chemistry: In situ infrared analysis of solid-phase organic reactions
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of special interest. This review highlights the methodology for in situ monitoring and analysis of solid phase organic reactions using IR analysis.
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Pivonka DE, Russell K, Gerot. Tools for combinatorial chemistry: in situ infrared analysis of solid-phase organic reactions. of special interest Appl Spec. 50:1996;1471-1478 This review highlights the methodology for in situ monitoring and analysis of solid phase organic reactions using IR analysis.
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(1996)
Appl Spec
, vol.50
, pp. 1471-1478
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Pivonka, D.E.1
Russell, K.2
Gerot3
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63
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0000683556
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Photoaccoustic FTIR spectroscopy, a nondestructive analysis of solid-phase organic chemistry
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Gosselin F, Di Renzo M, Ellis TH, Lubell WD. Photoaccoustic FTIR spectroscopy, a nondestructive analysis of solid-phase organic chemistry. J Org Chem. 61:1996;7980-7981.
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(1996)
J Org Chem
, vol.61
, pp. 7980-7981
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Gosselin, F.1
Di Renzo, M.2
Ellis, T.H.3
Lubell, W.D.4
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64
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0029926720
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Novel solution phase strategy for the synthesis of chemical libraries containing small organic molecules
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of outstanding interest. The solution synthesis of an iminodiacetic acid library is reported. Purification at each reaction step of the three step sequence was achieved by simple aqueous extraction allowing a library of around 1,000 compounds to be prepared.
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Boger DL, Cheng S, Comer DD, Williams JP, Myers PL. Novel solution phase strategy for the synthesis of chemical libraries containing small organic molecules. of outstanding interest J Am Chem Soc. 118:1996;2567-2573 The solution synthesis of an iminodiacetic acid library is reported. Purification at each reaction step of the three step sequence was achieved by simple aqueous extraction allowing a library of around 1,000 compounds to be prepared.
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(1996)
J Am Chem Soc
, vol.118
, pp. 2567-2573
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Boger, D.L.1
Cheng, S.2
Comer, D.D.3
Williams, J.P.4
Myers, P.L.5
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65
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0031029886
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Fluorous strategy: A fluorous-phase strategy for improving separation efficiency in organic synthesis
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of outstanding interest. This paper, along with Studer et al. 1997 [65] and Studer and Curran 1997 [66], describe the use of a fluorous phase strategy for improving separation efficiency in solution library synthesis. Organic molecules of interest can be rendered soluble in fluorocarbon solvents by attachment of a suitable perfluoro handle, thereby allowing separation.
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Studer A, Hadida S, Ferrito R, Sun-Young K, Jeger P, Wipf P, Curran DP. Fluorous strategy: a fluorous-phase strategy for improving separation efficiency in organic synthesis. of outstanding interest Science. 275:1997;823-826 This paper, along with Studer et al. 1997 [65] and Studer and Curran 1997 [66], describe the use of a fluorous phase strategy for improving separation efficiency in solution library synthesis. Organic molecules of interest can be rendered soluble in fluorocarbon solvents by attachment of a suitable perfluoro handle, thereby allowing separation.
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(1997)
Science
, vol.275
, pp. 823-826
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Studer, A.1
Hadida, S.2
Ferrito, R.3
Sun-Young, K.4
Jeger, P.5
Wipf, P.6
Curran, D.P.7
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66
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0001591221
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Fluorous synthesis: Fluorous protocols for the Ugi and Biginelli multicomponent condensations
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Studer A, Jeger P, Wipf P, Curran DP. Fluorous synthesis: fluorous protocols for the Ugi and Biginelli multicomponent condensations. J Org Chem. 62:1997;2917-2924.
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(1997)
J Org Chem
, vol.62
, pp. 2917-2924
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Studer, A.1
Jeger, P.2
Wipf, P.3
Curran, D.P.4
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67
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0031000561
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A strategic alternative to solid phase synthesis: Preparation of a small isoxazoline library by fluorous synthesis
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Studer A, Curran DP. A strategic alternative to solid phase synthesis: preparation of a small isoxazoline library by fluorous synthesis. Tetrahedron. 53:1997;6681-6696.
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(1997)
Tetrahedron
, vol.53
, pp. 6681-6696
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Studer, A.1
Curran, D.P.2
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68
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0031021840
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Ion-exchange resins for solution phase parallel synthesis of chemical libraries
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of special interest. Ion-exchange resins for solution phase parallel synthesis of chemical libraries facilitated the production of amide, ester and urea libraries.
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Gayo LM, Suto MJ. Ion-exchange resins for solution phase parallel synthesis of chemical libraries. of special interest Tetrahedron Lett. 38:1997;513-516 Ion-exchange resins for solution phase parallel synthesis of chemical libraries facilitated the production of amide, ester and urea libraries.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 513-516
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-
Gayo, L.M.1
Suto, M.J.2
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69
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0030607141
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Use of solid supported nucleophiles and electrophiles for the purification of non-peptide small molecule libraries
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of outstanding interest. Solid supported nucleophiles and electropiles are employed by the authors to expedite the work-up and purification of products from a variety of amine alkylations and acylations carried out in a parallel array format.
-
Kaldor SW, Siegel MG, Fritz JE, Dressman BA, Hahn PJ. Use of solid supported nucleophiles and electrophiles for the purification of non-peptide small molecule libraries. of outstanding interest Tetrahedron Lett. 37:1996;7193-7196 Solid supported nucleophiles and electropiles are employed by the authors to expedite the work-up and purification of products from a variety of amine alkylations and acylations carried out in a parallel array format.
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(1996)
Tetrahedron Lett
, vol.37
, pp. 7193-7196
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Kaldor, S.W.1
Siegel, M.G.2
Fritz, J.E.3
Dressman, B.A.4
Hahn, P.J.5
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70
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0030987922
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Polymer-supported quenching reagents for parallel synthesis
-
of outstanding interest. In a related approach to Kaldor et al. [68], the use of reactive species attached to solid phase support are used to quench excess reactants and remove known impurities. A pyrazole library synthesis exemplifies the approach.
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Booth RJ, Hodges JC. Polymer-supported quenching reagents for parallel synthesis. of outstanding interest J Am Chem Soc. 119:1997;4882-4886 In a related approach to Kaldor et al. [68], the use of reactive species attached to solid phase support are used to quench excess reactants and remove known impurities. A pyrazole library synthesis exemplifies the approach.
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(1997)
J Am Chem Soc
, vol.119
, pp. 4882-4886
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Booth, R.J.1
Hodges, J.C.2
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71
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0030952762
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Chemical library purification strategies based on principles of complementary molecular reactivity and molecular recognition
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of outstanding interest. The authors, essentially using the same concepts outlined by Kaldor et al. 1996 [68] and Booth and Hodges 1997 [69], report the sequestration of excess reactants, reagents and byproducts by complementary reactive intermediates tagged to resins. Examples of the techniques are illustrated with amine acylation, Moffat oxidation and Grignard reactions.
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Flynn DL, Crich JZ, Devraj RV, Hockerman SL, Parlow JJ, South MS, Woodward S. Chemical library purification strategies based on principles of complementary molecular reactivity and molecular recognition. of outstanding interest J Am Chem Soc. 119:1997;4874-4881 The authors, essentially using the same concepts outlined by Kaldor et al. 1996 [68] and Booth and Hodges 1997 [69], report the sequestration of excess reactants, reagents and byproducts by complementary reactive intermediates tagged to resins. Examples of the techniques are illustrated with amine acylation, Moffat oxidation and Grignard reactions.
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(1997)
J Am Chem Soc
, vol.119
, pp. 4874-4881
-
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Flynn, D.L.1
Crich, J.Z.2
Devraj, R.V.3
Hockerman, S.L.4
Parlow, J.J.5
South, M.S.6
Woodward, S.7
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72
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0029963887
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Postcondensation modifications of Ugi four-component condensation products: I-isocyano cyclohexene as a convertible isocyanide. Mechanism of conversion, synthesis of diverse structures and demonstration of resin capture
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of outstanding interest. Resin capture is a technique where the products of solution synthesis are trapped onto an appropriate solid support resin. Both the trapping step and subsequent cleavage of the products from the resin occur in very high yield, as demonstrated by this study utilizing the Ugi reaction.
-
Keating TA, Armstrong RW. Postcondensation modifications of Ugi four-component condensation products: I-isocyano cyclohexene as a convertible isocyanide. Mechanism of conversion, synthesis of diverse structures and demonstration of resin capture. of outstanding interest J Am Chem Soc. 118:1996;2574-2583 Resin capture is a technique where the products of solution synthesis are trapped onto an appropriate solid support resin. Both the trapping step and subsequent cleavage of the products from the resin occur in very high yield, as demonstrated by this study utilizing the Ugi reaction.
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(1996)
J Am Chem Soc
, vol.118
, pp. 2574-2583
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Keating, T.A.1
Armstrong, R.W.2
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73
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0031098534
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Organic synthesis on soluble polymer supports; Liquid-phase methodologies
-
of outstanding interest. The authors provide a comprehensive review of the use of polyethylene glycol resin in library synthesis. Polyethylene glycol offers the attribute of both solution synthesis followed by precipitation to give a solid phase medium which can be readily purified to give ultimately a clean product on cleavage.
-
Gravert DJ, Janda KD. Organic synthesis on soluble polymer supports; liquid-phase methodologies. of outstanding interest Chem Rev. 97:1997;489-509 The authors provide a comprehensive review of the use of polyethylene glycol resin in library synthesis. Polyethylene glycol offers the attribute of both solution synthesis followed by precipitation to give a solid phase medium which can be readily purified to give ultimately a clean product on cleavage.
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(1997)
Chem Rev
, vol.97
, pp. 489-509
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Gravert, D.J.1
Janda, K.D.2
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74
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0029905917
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Rapid combinatorial synthesis of aminoglycoside antibiotic mimetics: Use of a polyethylene glycol-linked amine and a neamine-derived aldehyde in multiple component condensation as a strategy for the discovery of new inhibitors of the HIV RNA rev responsive element
-
of outstanding interest. The utilization of polyethylene glycol resin in the synthesis of a library of complex neomycin B derivatives as potential inhibitors of the HIV RNA Rev responsive element is described.
-
Park WKC, Auer M, Jakshe H, Wong C-H. Rapid combinatorial synthesis of aminoglycoside antibiotic mimetics: use of a polyethylene glycol-linked amine and a neamine-derived aldehyde in multiple component condensation as a strategy for the discovery of new inhibitors of the HIV RNA rev responsive element. of outstanding interest J Am Chem Soc. 118:1996;10150-10155 The utilization of polyethylene glycol resin in the synthesis of a library of complex neomycin B derivatives as potential inhibitors of the HIV RNA Rev responsive element is described.
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(1996)
J Am Chem Soc
, vol.118
, pp. 10150-10155
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-
Park, W.K.C.1
Auer, M.2
Jakshe, H.3
Wong C-H4
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