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1
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0031116628
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Combinatorial chemistry and new drugs
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April
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Ellman JA, Plunkett MJ: Combinatorial chemistry and new drugs. Sci Am 1997, April:68-73. This describes the synthesis of small-molecule libraries for lead optimization and lead generation as an important component of drug discovery.
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Sci Am
, pp. 68-73
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Ellman, J.A.1
Plunkett, M.J.2
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2
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0030939592
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Combinatorial chemistry in drug discovery
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Hogan JG Jr: Combinatorial chemistry in drug discovery. Nat Biotechnol 1997, 15:328-330. This describes the synthesis of small-molecule libraries for lead optimization and lead generation as an important component of drug discovery.
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Nat Biotechnol
, vol.15
, pp. 328-330
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Hogan J.G., Jr.1
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3
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0029904314
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Parallel-compound synthesis: Methodology for accelerating drug discovery
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Se way CN, Terrett NK: Parallel-compound synthesis: methodology for accelerating drug discovery. Bioorg Med Chem 1996, 4:645-654. This describes the synthesis of small-molecule libraries for lead optimization and lead generation as an important component of drug discovery.
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Bioorg Med Chem
, vol.4
, pp. 645-654
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Se Way, C.N.1
Terrett, N.K.2
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4
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0000074870
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Strategy and tactics in combinatorial organic synthesis. Applications to drug discovery
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Gordon EM, Gallop MA, Patel DV: Strategy and tactics in combinatorial organic synthesis. Applications to drug discovery. Accounts Chem Res 1996, 29:144-154. This describes the synthesis of small-molecule libraries for lead optimization and lead generation as an important component of drug discovery.
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(1996)
Accounts Chem Res
, vol.29
, pp. 144-154
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Gordon, E.M.1
Gallop, M.A.2
Patel, D.V.3
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5
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0028031367
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Formation of carbon-carbon bond on solid support: Application of the Stille reaction
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Deshpande MS: Formation of carbon-carbon bond on solid support: application of the Stille reaction. Tetrahedron Lett 1994, 33:5613-5614.
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(1994)
Tetrahedron Lett
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Deshpande, M.S.1
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7
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0028088788
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Biaryl synthesis via Suzuki coupling on a solid support
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Frenette R, Friesen RW: Biaryl synthesis via Suzuki coupling on a solid support Tetrahedron Lett 1994, 35:9177-9180.
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(1994)
Tetrahedron Lett
, vol.35
, pp. 9177-9180
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Frenette, R.1
Friesen, R.W.2
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8
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0000428035
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Synthesis of indoles via palladium-catalyzed heteroannulation of internal alkynes
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Larock RC, Yum EK: Synthesis of indoles via palladium-catalyzed heteroannulation of internal alkynes. J Am Chem Soc 1991, 113:2439-2442.
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J Am Chem Soc
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Larock, R.C.1
Yum, E.K.2
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9
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0030906033
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Synthesis of trisubstituted indoles on the solid phase via palladium-mediated heteroannulation of internal alkynes
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Zhang HC, Brumfield KK, Maryanoff BE: Synthesis of trisubstituted indoles on the solid phase via palladium-mediated heteroannulation of internal alkynes. Tetrahedron Lett 1997, 38:2439-2442.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 2439-2442
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Zhang, H.C.1
Brumfield, K.K.2
Maryanoff, B.E.3
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10
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0031592570
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Solid-phase synthesis of indoles using the palladium-catalysed coupling of alkynes with iodoaniline derivatives
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Fagnola MC, Candiani H, Visentin G, Cabri W, Zarini F, Mongelli N, Bedeshi A: Solid-phase synthesis of indoles using the palladium-catalysed coupling of alkynes with iodoaniline derivatives. Tetrahedron Lett 1997, 38:2307-2310.
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(1997)
Tetrahedron Lett
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Fagnola, M.C.1
Candiani, H.2
Visentin, G.3
Cabri, W.4
Zarini, F.5
Mongelli, N.6
Bedeshi, A.7
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11
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0031592575
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Solid-phase synthesis of benzofurans via the palladium-catalysed heteroannulation of acetylenes
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Fancelli D, Fagnola MC, Severino D, Bedeshi A: Solid-phase synthesis of benzofurans via the palladium-catalysed heteroannulation of acetylenes. Tetrahedron Lett 1997, 33:2311-2314.
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(1997)
Tetrahedron Lett
, vol.33
, pp. 2311-2314
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Fancelli, D.1
Fagnola, M.C.2
Severino, D.3
Bedeshi, A.4
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12
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0030793233
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Macrocyclization on solid support using Heck reaction
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2. Akaji K, Kiso Y: Macrocyclization on solid support using Heck reaction. Tetrahedron Lett 1997, 38:5185-5188.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 5185-5188
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Akaji, K.1
Kiso, Y.2
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13
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0030879776
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Synthesis of 2-oxindole derivatives via the intramolecular Heck reaction on solid support
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Arumugam V, Routledge A, Abell C, Balasubramanian S: Synthesis of 2-oxindole derivatives via the intramolecular Heck reaction on solid support. Tetrahedron Lett 1997, 38:6473-6476.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 6473-6476
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Arumugam, V.1
Routledge, A.2
Abell, C.3
Balasubramanian, S.4
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14
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0031575574
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A new approach to the solid-phase Suzuki coupling reaction
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Piettre SR, Baltzer S: A new approach to the solid-phase Suzuki coupling reaction. Tetrahedron Lett 1997, 38:1197-1200.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 1197-1200
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Piettre, S.R.1
Baltzer, S.2
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15
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0346933363
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Palladium(0)-catalyzed cross-coupling reactions of alkoxydiboron with haloarenes: A direct procedure for arylboronic esters
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Ishiyama T, Murata M, Miyaura N: Palladium(0)-catalyzed cross-coupling reactions of alkoxydiboron with haloarenes: a direct procedure for arylboronic esters. J Org Chem 1991, 56:3763-3768.
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(1991)
J Org Chem
, vol.56
, pp. 3763-3768
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Ishiyama, T.1
Murata, M.2
Miyaura, N.3
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16
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0030062225
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Synthesis of tetrasubstituted ethylenes on solid support via resin capture
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Brown SD, Armstrong RW: Synthesis of tetrasubstituted ethylenes on solid support via resin capture. J Am Chem Soc 1996, 118:6331-6332.
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(1996)
J Am Chem Soc
, vol.118
, pp. 6331-6332
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Brown, S.D.1
Armstrong, R.W.2
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17
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0031008230
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Two methods for the preparation of 2-cyclohexenones from resin-bound 1,3-cyclohexanedione
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Fraley ME, Rubina RS: Two methods for the preparation of 2-cyclohexenones from resin-bound 1,3-cyclohexanedione. Tetrahedron Lett 1997, 38:3365-3368.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 3365-3368
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Fraley, M.E.1
Rubina, R.S.2
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18
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0001083115
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Solid-phase synthesis of 4-arylazetidin-2-ones via Suzuki and Heck cross-coupling reactions
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Ruhland B, Bombrun A, Gallop GA: Solid-phase synthesis of 4-arylazetidin-2-ones via Suzuki and Heck cross-coupling reactions. J Org Chem 1997, 62:7820-7826. The authors describe the use of Suzuki and Heck cross-coupling reactions for diversification of haloaryl-β-lactams.
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(1997)
J Org Chem
, vol.62
, pp. 7820-7826
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Ruhland, B.1
Bombrun, A.2
Gallop, G.A.3
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19
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33748621833
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A simple catalytic method for the conversion of aryl bromides to arylamines
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Guram AS, Rennels RA, Buchwald SL: A simple catalytic method for the conversion of aryl bromides to arylamines. Agnew Chem Int Ed 1 995, 34:1348-1352.
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Agnew Chem Int Ed
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, pp. 1348-1352
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Guram, A.S.1
Rennels, R.A.2
Buchwald, S.L.3
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20
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0029044538
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Palladium-catalyzed synthesis of arylamines from aryl halides: Mechanistic studies lead to coupling in the absence of tin reagents
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Louie J, Hartwig JF: Palladium-catalyzed synthesis of arylamines from aryl halides: mechanistic studies lead to coupling in the absence of tin reagents. Tetrahedron Lett 1995, 36:3609-3614.
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(1995)
Tetrahedron Lett
, vol.36
, pp. 3609-3614
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Louie, J.1
Hartwig, J.F.2
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21
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0030599273
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Solid phase synthesis of aryl amines via palladium catalyzed amination of resin-bound aromatic bromides
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Ward YD, Farina F: Solid phase synthesis of aryl amines via palladium catalyzed amination of resin-bound aromatic bromides. Tetrahedron Lett 1996, 37:6993-6996.
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(1996)
Tetrahedron Lett
, vol.37
, pp. 6993-6996
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Ward, Y.D.1
Farina, F.2
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23
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0029883219
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Palladium-mediated three-component coupling strategy for the solid-phase synthesis of tropane derivatives
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Koh JS, Ellman JA; Palladium-mediated three-component coupling strategy for the solid-phase synthesis of tropane derivatives. J Org Chem 1996, 61:4494-4495. The authors describe a three-component coupling strategy for synthesis of tropane derivatives.
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(1996)
J Org Chem
, vol.61
, pp. 4494-4495
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Koh, J.S.1
Ellman, J.A.2
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24
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0030605889
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Aryl-aryl coupling on a solid support using zinc organic reagents and palladium catalysis
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Marquais S, Arlt M: Aryl-aryl coupling on a solid support using zinc organic reagents and palladium catalysis. Tetrahedron Lett 1996, 31:5491-5494.
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(1996)
Tetrahedron Lett
, vol.31
, pp. 5491-5494
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Marquais, S.1
Arlt, M.2
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25
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0030977733
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Solid-phase synthesis of peptide mimetics with (E)-alkene amide bond replacements derived from alkenylaziridines
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Wipf P, Henninger TC: Solid-phase synthesis of peptide mimetics with (E)-alkene amide bond replacements derived from alkenylaziridines. J Org Chem 1997, 62:1586-1587.
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(1997)
J Org Chem
, vol.62
, pp. 1586-1587
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Wipf, P.1
Henninger, T.C.2
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26
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0030817243
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'Traceless' solid-phase synthesis of furans via 1,3-dipolar cycloaddition reactions of isomunchnones
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Gowravaram MR, Gallop MA: 'Traceless' solid-phase synthesis of furans via 1,3-dipolar cycloaddition reactions of isomunchnones. Tetrahedron Lett 1997, 38:6973-6976. The authors describe the rhodium(II)-catalyzed 1,3-dipolar cycloaddition reaction of the alkyme diesler dipolarophiles with resin-bound carbonyl ylides, prepared on TentaGel™ resin.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 6973-6976
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Gowravaram, M.R.1
Gallop, M.A.2
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27
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0030661784
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A chemoselective rhodium(II) mediated solid phase 1,3-dipolar cycloaddition and its application to a thermally self-cleaving furan scaffold
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Whitehouse DL, Nelson Jr. KH, Savinov SN, Austin DJ: A chemoselective rhodium(II) mediated solid phase 1,3-dipolar cycloaddition and its application to a thermally self-cleaving furan scaffold. Tetrahedron Lett 1997, 38:7139-7142. The authors describe the rhodium(II)-catalyzed 1,3-dipolar cycloaddition reaction of the alkyme diester dipolarophiles with resin-bound carbonyl ylides, prepared on Wang resin.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 7139-7142
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Whitehouse, D.L.1
Nelson K.H., Jr.2
Savinov, S.N.3
Austin, D.J.4
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28
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0030569374
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Solid phase ring-closing metathesis: Cyclization/cleavage approach towards a seven membered cycloolefin
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van Maarseveen JH, den Hartog JAJ, Engelen V, Finner E, Visser G, Kruse CG: Solid phase ring-closing metathesis: cyclization/cleavage approach towards a seven membered cycloolefin. Tetrahedron Lett 1996, 37:8249-8252, The authors describe the application of solid-phase ring closing metathesis Io yield cycloolefins in solution, without traceable polymer linker contamina-tion.
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(1996)
Tetrahedron Lett
, vol.37
, pp. 8249-8252
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Van Maarseveen, J.H.1
Den Hartog, J.A.J.2
Engelen, V.3
Finner, E.4
Visser, G.5
Kruse, C.G.6
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29
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0030693762
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Solid phase heterocyclic synthesis via ring closing metathesis: Traceless linking and cyclative cleavage through a carbon-carbon double bond
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Piscopio AD, Miller JF, Koch K: Solid phase heterocyclic synthesis via ring closing metathesis: traceless linking and cyclative cleavage through a carbon-carbon double bond. Tetrahedron Lett 1997, 38:7143-7146. Here, Friedlinger lactam was synthesized from cinnamyl alcohol resin in four steps.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 7143-7146
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Piscopio, A.D.1
Miller, J.F.2
Koch, K.3
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30
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0001847655
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Cleavage of styrene derivatives from a solid support by ring closing olefin metathesis
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Peters J-U, Blechert S: Cleavage of styrene derivatives from a solid support by ring closing olefin metathesis. Synlett 1997:348-350.
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(1997)
Synlett
, pp. 348-350
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Peters, J.-U.1
Blechert, S.2
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31
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0029860486
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Application of ring-closing metathesis to the synthesis of rigidified amino acids and peptides
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Miller SJ, Blackwell HE, Grubbs RH: Application of ring-closing metathesis to the synthesis of rigidified amino acids and peptides. J Am Chem Soc 1996, 118:9606-9614. The authors describe the utilization of the ring-closure metathesis reaction in a non-cleaving sense.
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(1996)
J Am Chem Soc
, vol.118
, pp. 9606-9614
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Miller, S.J.1
Blackwell, H.E.2
Grubbs, R.H.3
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32
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0031576842
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Solution-phase combinatorial synthesis via the olefin metathesis reaction
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Boger DL, Chai W, Ozer RS, Andersson C-M: Solution-phase combinatorial synthesis via the olefin metathesis reaction. Bioorg Med Chem Lett 1997, 7:463-468.
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(1997)
Bioorg Med Chem Lett
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, pp. 463-468
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Boger, D.L.1
Chai, W.2
Ozer, R.S.3
Andersson, C.-M.4
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33
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0029978630
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Solid phase synthesis of azabicyclo[4,3,0]nonen-8-one amino acid derivatives via intramolecular Pauson-Khand cyclization
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Bolton GL: Solid phase synthesis of azabicyclo[4,3,0]nonen-8-one amino acid derivatives via intramolecular Pauson-Khand cyclization. Tetrahedron Lett 1996, 37:3433-3436. Here, the authors describe the use of the Pauson-Khand cyclization reaction for the synthesis of libraries of bicyclic, constrained amino acids on solid support.
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(1996)
Tetrahedron Lett
, vol.37
, pp. 3433-3436
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Bolton, G.L.1
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34
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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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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. Tetrahedron 1997, 53:6611-6634. The authors also describe the use of the Pauson-Khand cyclization reaction for the construction of libraries of bicyclic, constrained amino acids on solid support.
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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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35
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0030998282
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Polymer-supported synthesis as a tool for improving chemoselectivity: Pauson-Khand reaction
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Kurth MJ, Spitzer JL Schore NE, Najdi SD: Polymer-supported synthesis as a tool for improving chemoselectivity: Pauson-Khand reaction. Tetrahedron 1997, 53:6791-6808.
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(1997)
Tetrahedron
, vol.53
, pp. 6791-6808
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Kurth, M.J.1
Spitzer, J.L.2
Schore, N.E.3
Najdi, S.D.4
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36
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0029813591
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A new methodology for combinatorial synthesis. Preparation of diverse quinoline derivatives using a novel polymer-supported scandium catalyst
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Kobayashi S, Nagayama S: A new methodology for combinatorial synthesis. Preparation of diverse quinoline derivatives using a novel polymer-supported scandium catalyst. J Am Chem Soc 1996, 118:8977-8978.
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(1996)
J Am Chem Soc
, vol.118
, pp. 8977-8978
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Kobayashi, S.1
Nagayama, S.2
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37
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0030605818
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Aldol reactions on solid phase. Sc(otf)-catalyzed aldol reactions of polymer-supported silyl enol ethers with aldehydes providing convenient methods for the preparation of 1,3-diol, β-hydroxy carboxylic acid, and β-hydroxy aldehyde libraries
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Kobayashi S, Hachiya I, Yasuda M: Aldol reactions on solid phase. Sc(otf)-catalyzed aldol reactions of polymer-supported silyl enol ethers with aldehydes providing convenient methods for the preparation of 1,3-diol, β-hydroxy carboxylic acid, and β-hydroxy aldehyde libraries. Tetrahderon Lett 1996, 37:5569-5572. The authors describe the use of scandium triflate for the synthesis of 1,3-diols on solid support.
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(1996)
Tetrahderon Lett
, vol.37
, pp. 5569-5572
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Kobayashi, S.1
Hachiya, I.2
Yasuda, M.3
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38
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0029883736
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Polymer-supported silyl enol ethers, Synthesis and reactions with imines for the preparation of an amino alcohol library
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Kobayashi S, Hachiya I, Suzuki S, Moriwaki M: Polymer-supported silyl enol ethers, Synthesis and reactions with imines for the preparation of an amino alcohol library. Tetrahedron Lett 1996, 37:2809-2812. The authors describe the construction of β-amino alcohol libraries via scandium triflale-catalyzed addition of polymer-supported silyl enol ethers to imines.
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(1996)
Tetrahedron Lett
, vol.37
, pp. 2809-2812
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Kobayashi, S.1
Hachiya, I.2
Suzuki, S.3
Moriwaki, M.4
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39
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0030597207
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Parallel synthesis using mannich-type three-component reactions and 'field synthesis' for the construction of an amino alcohol library
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Kobayashi S, Moriwaki M, Akiyama R, Suzuki S, Hachiya I: Parallel synthesis using mannich-type three-component reactions and 'field synthesis' for the construction of an amino alcohol library. Tetrahderon Lett 1996, 37:7783-7786. The authors describe the construction of libraries of ß-amino alcohol via scandium triflate-catalyzed addition of polymer-supported silyl enol ethers to imines.
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(1996)
Tetrahderon Lett
, vol.37
, pp. 7783-7786
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Kobayashi, S.1
Moriwaki, M.2
Akiyama, R.3
Suzuki, S.4
Hachiya, I.5
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40
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0030921272
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Solid phase synthesis of 2,3-dihydro-4-pyridones: Reaction of Danishefsky's diene with polymer-bound imines
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Wang Y, Wilson SR; Solid phase synthesis of 2,3-dihydro-4-pyridones: reaction of Danishefsky's diene with polymer-bound imines. Tetrahedron Lett 1997, 38:4021-4024.
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(1997)
Tetrahedron Lett
, vol.38
, pp. 4021-4024
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Wang, Y.1
Wilson, S.R.2
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41
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0028907801
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Trimethylorthoformate: A mild and effective dehydrating reagent for solution and solid phase imine formation
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Look GC, Murphy M, Campbell DA, Gallop MA: Trimethylorthoformate: a mild and effective dehydrating reagent for solution and solid phase imine formation. Tetrahedron Lett 1995, 36:2937-2940.
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(1995)
Tetrahedron Lett
, vol.36
, pp. 2937-2940
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Look, G.C.1
Murphy, M.2
Campbell, D.A.3
Gallop, M.A.4
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