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1
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0001277768
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The synthesis of amino acids by 1,3-dipolar cycloadditions of azomethine ylides
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Kraus G.A., Nagy J.O. The synthesis of amino acids by 1,3-dipolar cycloadditions of azomethine ylides. Tetrahedron. 41:1985;3537-3545.
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(1985)
Tetrahedron
, vol.41
, pp. 3537-3545
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Kraus, G.A.1
Nagy, J.O.2
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2
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33845375114
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Multicomponent one-pot annulations forming three to six bonds
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Posner G.H. Multicomponent one-pot annulations forming three to six bonds. Chem Rev. 86:1986;831-834.
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(1986)
Chem Rev
, vol.86
, pp. 831-834
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Posner, G.H.1
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3
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0028757621
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Multicomponent reactions in organic chemistry
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Ugi I., Dömling A., Hoerl W. Multicomponent reactions in organic chemistry. Endeavour. 18:1994;115-122.
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(1994)
Endeavour
, vol.18
, pp. 115-122
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Ugi, I.1
Dömling, A.2
Hoerl, W.3
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4
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0000512227
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Multiple-component condensation strategies for combinatorial library synthesis
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Armstrong R.W., Combs A.P., Tempest P.A., Brown S.D., Keating T.A. Multiple-component condensation strategies for combinatorial library synthesis. Accounts Chem Res. 29:1996;123-131.
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(1996)
Accounts Chem Res
, vol.29
, pp. 123-131
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Armstrong, R.W.1
Combs, A.P.2
Tempest, P.A.3
Brown, S.D.4
Keating, T.A.5
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5
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33749872930
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Perspektiven von Multikomponentenreaktionen und deren Bibliotheken
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[Title translation: Perspectives of multi-component reactions and their libraries.]
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Ugi I. Perspektiven von Multikomponentenreaktionen und deren Bibliotheken. J Prakt Chem. 339:1997;499-516. [Title translation: Perspectives of multi-component reactions and their libraries.].
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(1997)
J Prakt Chem
, vol.339
, pp. 499-516
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Ugi, I.1
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6
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0032035067
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Isocyanide based multi component reactions in combinatorial chemistry
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Dömling A. Isocyanide based multi component reactions in combinatorial chemistry. Comb Chem High Throughput Screen. 1:1999;1.
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(1999)
Comb Chem High Throughput Screen
, vol.1
, pp. 1
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Dömling, A.1
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7
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84980922405
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Isonitrile 2. Reaktionen von Isonitrilen mit Carbonylverbindungen, Aminen und Stickstoffwasserstoffsäure
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[Title translation: Isocyanides 2. Reactions of isocyanides, carbonyl compounds, amines and hydrogenazid.]
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Ugi I., Steinbrückner C. Isonitrile 2. Reaktionen von Isonitrilen mit Carbonylverbindungen, Aminen und Stickstoffwasserstoffsäure. Chem Ber. 94:1961;734-742. [Title translation: Isocyanides 2. Reactions of isocyanides, carbonyl compounds, amines and hydrogenazid.].
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(1961)
Chem Ber
, vol.94
, pp. 734-742
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Ugi, I.1
Steinbrückner, C.2
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8
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0032541686
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® piperazine intermediate
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The paper describes attempts to find a shorter and more efficient MCR synthetic route to Merck's HIV protease inhibitor CRIXIVAN, a compound already on the market, which is normally synthesised by a long divergent route
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® piperazine intermediate. Tetrahedron Lett. 39:1998;6823-6826. The paper describes attempts to find a shorter and more efficient MCR synthetic route to Merck's HIV protease inhibitor CRIXIVAN, a compound already on the market, which is normally synthesised by a long divergent route.
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(1998)
Tetrahedron Lett
, vol.39
, pp. 6823-6826
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Rossen, K.1
Pye, P.J.2
Dimichele, L.M.3
Voante, R.P.4
Reider, P.J.5
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9
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0033554026
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Total synthesis of motuporin (nodularin-V)
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This paper demonstrates the beneficial use of MCRs in the total synthesis of complex natural products
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Bauer S.M., Armstrong R.W. Total synthesis of motuporin (nodularin-V). J Am Chem Soc. 121:1999;6355-6366. This paper demonstrates the beneficial use of MCRs in the total synthesis of complex natural products.
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(1999)
J Am Chem Soc
, vol.121
, pp. 6355-6366
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Bauer, S.M.1
Armstrong, R.W.2
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10
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30244439892
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Neue Reaktionen für die Kombinatorische Chemie
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[Title translation: New reactions for combinatorial chemistry.]
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Lacke O., Weber L. Neue Reaktionen für die Kombinatorische Chemie. Chimia. 50:1996;445-447. [Title translation: New reactions for combinatorial chemistry.].
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(1996)
Chimia
, vol.50
, pp. 445-447
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Lacke, O.1
Weber, L.2
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13
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0030603133
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Ugi reaction with trifunctional α-amino acids, aldehydes isocyanides and alcohols
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Ugi I., Demharter A., Hörl A., Schmid T. Ugi reaction with trifunctional α-amino acids, aldehydes isocyanides and alcohols. Tetrahedron. 52:1996;11657-11664.
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(1996)
Tetrahedron
, vol.52
, pp. 11657-11664
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Ugi, I.1
Demharter, A.2
Hörl, A.3
Schmid, T.4
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14
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0039944586
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A versatile multi-component one-pot thiazole synthesis
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For the first time, a versatile MCR of thiazoles from four starting materials is described. The 2,4-disubstituted thiazoles have the same substitution pattern as many naturally occurring thiazoles
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Heck S., Dömling A. A versatile multi-component one-pot thiazole synthesis. Synlett. 2000;424-426. For the first time, a versatile MCR of thiazoles from four starting materials is described. The 2,4-disubstituted thiazoles have the same substitution pattern as many naturally occurring thiazoles.
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(2000)
Synlett
, pp. 424-426
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Heck, S.1
Dömling, A.2
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15
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0033525660
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Preparation of trcyclic nitrogen heterocycles via tandem four-component condensation/intamolecular Diels-Alder reaction
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This work describes the generation of libaries of complex tricycles by using MCRs and Diels-Alder reactions both in solid and solution phase
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Paulvannan K. Preparation of trcyclic nitrogen heterocycles via tandem four-component condensation/intamolecular Diels-Alder reaction. Tetrahedron Lett. 40:1999;1851-1854. This work describes the generation of libaries of complex tricycles by using MCRs and Diels-Alder reactions both in solid and solution phase.
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(1999)
Tetrahedron Lett
, vol.40
, pp. 1851-1854
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Paulvannan, K.1
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16
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33749842822
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Optimization of the biological activity of combinatorial compound libraries with a genetic algorithm
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Weber L., Waltbaum S., Broger C., Gubernator K. Optimization of the biological activity of combinatorial compound libraries with a genetic algorithm. Angew Chem Int Ed Engl. 34:1995;2280-2282.
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(1995)
Angew Chem Int Ed Engl
, vol.34
, pp. 2280-2282
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Weber, L.1
Waltbaum, S.2
Broger, C.3
Gubernator, K.4
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17
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0032580464
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Synthesis of rigid hydrophobic tetrazoles using an Ugi multi-component heterocyclic condensation
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This paper demonstrates the use of a highly convergent four-component, one-pot reaction for the synthesis of a new bicyclic tetrazole scaffold. Libraries in the 10,000-compound range could thus be generated
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Bienaymé H., Bouzid K. Synthesis of rigid hydrophobic tetrazoles using an Ugi multi-component heterocyclic condensation. Tetrahedron Lett. 39:1998;2735-2738. This paper demonstrates the use of a highly convergent four-component, one-pot reaction for the synthesis of a new bicyclic tetrazole scaffold. Libraries in the 10,000-compound range could thus be generated.
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(1998)
Tetrahedron Lett
, vol.39
, pp. 2735-2738
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Bienaymé, H.1
Bouzid, K.2
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18
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0032578740
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Application of N-BOC-diamines for the solution phase synthesis of ketopiperazine libraries utilizing a Ugi/de-BOC/cyclisation (UDB) strategy
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Libraries with the scaffold of ketopiperazine, dihydroquinoxalinone and 1,4-benzodiazepine can be generated by using MCRs with appropriately protected building blocks. Thus, first the U-MCR takes place, the amide of the former isocyanide is protected with N-tert-butoxycarbonyl (Boc) and deprotection of the substituents results in a heterocyclic structure. In this variation, only the isocyanide carbon is still present in the products. This procedure is particularly suitable for the generation of large libraries either in solutions, or in the solid phase
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Hulme C., Peng J., Louridas B., Menard B., Krolikowski P., Kumar N.V. Application of N-BOC-diamines for the solution phase synthesis of ketopiperazine libraries utilizing a Ugi/de-BOC/cyclisation (UDB) strategy. Tetrahedron Lett. 39:1998;8047-8050. Libraries with the scaffold of ketopiperazine, dihydroquinoxalinone and 1,4-benzodiazepine can be generated by using MCRs with appropriately protected building blocks. Thus, first the U-MCR takes place, the amide of the former isocyanide is protected with N-tert-butoxycarbonyl (Boc) and deprotection of the substituents results in a heterocyclic structure. In this variation, only the isocyanide carbon is still present in the products. This procedure is particularly suitable for the generation of large libraries either in solutions, or in the solid phase.
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(1998)
Tetrahedron Lett
, vol.39
, pp. 8047-8050
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Hulme, C.1
Peng, J.2
Louridas, B.3
Menard, B.4
Krolikowski, P.5
Kumar, N.V.6
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19
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84952146812
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Studies on isocyanides and related compounds: Synthesis of oxazole derivatives via a Passerini reaction
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Bossio R., Marcaccini S., Pepino R. Studies on isocyanides and related compounds: synthesis of oxazole derivatives via a Passerini reaction. Liebigs Ann Chem. 1991;1107-1108.
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(1991)
Liebigs Ann Chem
, pp. 1107-1108
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Bossio, R.1
Marcaccini, S.2
Pepino, R.3
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20
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0033538596
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Passerini and Ugi reactions of benzyl and acetyl protected isocyanoglucoses
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Glycosylated peptides are ubiquitous in all living cells. They play important roles in processes such as cell-cell recognition, pathogen recognition, cell migration and immune response. In order to understand and modify these processes, there is a strong need for easy synthesis of glycosylated peptides and their libraries. In this article, the easy preparation of such compounds by MCRs, with the help of isocyanosugars, is described
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Ziegler T., Kaiser H-J., Schlömer R., Koch C. Passerini and Ugi reactions of benzyl and acetyl protected isocyanoglucoses. Tetrahedron. 55:1999;8397-8408. Glycosylated peptides are ubiquitous in all living cells. They play important roles in processes such as cell-cell recognition, pathogen recognition, cell migration and immune response. In order to understand and modify these processes, there is a strong need for easy synthesis of glycosylated peptides and their libraries. In this article, the easy preparation of such compounds by MCRs, with the help of isocyanosugars, is described.
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(1999)
Tetrahedron
, vol.55
, pp. 8397-8408
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Ziegler, T.1
Kaiser, H.-J.2
Schlömer, R.3
Koch, C.4
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21
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0029905917
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Rapid combination of aminoglycid antibiotic mimetics: Use of a polyethyleneglycol linked neamine derived aldehyde in multiple compound condensation as an assay strategy for the discovery of new inhibitors of the HIV-RNA response element
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Park W.K.C., Auer M., Jaschke H., Wong C.H. Rapid combination of aminoglycid antibiotic mimetics: use of a polyethyleneglycol linked neamine derived aldehyde in multiple compound condensation as an assay strategy for the discovery of new inhibitors of the HIV-RNA response element. J Am Chem Soc. 118:1996;10150-10155.
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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
Jaschke, H.3
Wong, C.H.4
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22
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0033521568
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An access to glycoconjugate libraries through multicomponent reactions
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The synthesis of pseudo-oligosaccharides by an MCR are described. In one example, four different monosaccharides, each bearing one functionality of the Ugi-reaction, are reacted in one-pot to give a tetrasaccharide
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Lockhoff O. An access to glycoconjugate libraries through multicomponent reactions. Angew Chem Int Ed Engl. 37:1998;3436-3439. The synthesis of pseudo-oligosaccharides by an MCR are described. In one example, four different monosaccharides, each bearing one functionality of the Ugi-reaction, are reacted in one-pot to give a tetrasaccharide.
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(1998)
Angew Chem Int Ed Engl
, vol.37
, pp. 3436-3439
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Lockhoff, O.1
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23
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0032563923
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A facile synthesis of N-carbamoylmethyl-α-aminobutyrolactones by the Ugi multicomponent condensation reaction
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Libraries of γ-lactames with three points of diversity are described
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Park S.J., Keum G., Kang S.B., Hoh H.Y., Kim Y. A facile synthesis of N-carbamoylmethyl-α-aminobutyrolactones by the Ugi multicomponent condensation reaction. Tetrahedron Lett. 39:1998;7109-7112. Libraries of γ-lactames with three points of diversity are described.
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(1998)
Tetrahedron Lett
, vol.39
, pp. 7109-7112
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Park, S.J.1
Keum, G.2
Kang, S.B.3
Hoh, H.Y.4
Kim, Y.5
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24
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0032564005
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Dibenzo-1,5-diazocine-2,6-dione, 2-iminoindolin-3-one and N-(carbamoylmethyl)-aminobenzoic acid ester from aminobenzoic acid by multicomponent reactions
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The reactions of p-aminobenzoic acid with aldehydes and isocyanides and their libraries are described
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Ebert B.M., Ugi I., Grosche M., Herdtweck E., Herrmann W.A. Dibenzo-1,5-diazocine-2,6-dione, 2-iminoindolin-3-one and N-(carbamoylmethyl)-aminobenzoic acid ester from aminobenzoic acid by multicomponent reactions. Tetrahedron. 54:1998;11887-11898. The reactions of p-aminobenzoic acid with aldehydes and isocyanides and their libraries are described.
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(1998)
Tetrahedron
, vol.54
, pp. 11887-11898
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Ebert, B.M.1
Ugi, I.2
Grosche, M.3
Herdtweck, E.4
Herrmann, W.A.5
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25
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0001560402
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MCR 6: Chiral 2,6-piperazinediones via Ugi reactions with α-amino acids, carbonyl compounds, isocyanides and alcohols
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The synthesis of spirocyclic piperazine diones and their libraries is described
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Ugi I., Hörl W., Hanusch C., Schmid T., Herdtweck E. MCR 6: chiral 2,6-piperazinediones via Ugi reactions with α-amino acids, carbonyl compounds, isocyanides and alcohols. Heterocycles. 47:1998;965-975. The synthesis of spirocyclic piperazine diones and their libraries is described.
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(1998)
Heterocycles
, vol.47
, pp. 965-975
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Ugi, I.1
Hörl, W.2
Hanusch, C.3
Schmid, T.4
Herdtweck, E.5
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26
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0032487905
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Five-component synthesis of marimastat analogues
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Metalloproteinases are emmergent new targets in the fields of cancer and inflammatory diseases. Natural products, such as Marimastat, are know that are inhibitors. In this study libraries of metalloproteinase inhibitors were synthesised by MCRs
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Patel S., Saroglou L., Floyd C.D., Miller A., Whittaker M. Five-component synthesis of marimastat analogues. Tetrahedron Lett. 39:1998;8333-8334. Metalloproteinases are emmergent new targets in the fields of cancer and inflammatory diseases. Natural products, such as Marimastat, are know that are inhibitors. In this study libraries of metalloproteinase inhibitors were synthesised by MCRs.
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(1998)
Tetrahedron Lett
, vol.39
, pp. 8333-8334
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Patel, S.1
Saroglou, L.2
Floyd, C.D.3
Miller, A.4
Whittaker, M.5
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27
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0033594360
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Identification of highly selective inhibitors of collagenase-1 from combinatorial libraries of diketopiperazines
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The synthesis of nanomolar inhibitors of collagenase-I, with a high selectivity over gelatinase and stromelysine, is described with a diketopiperazine backbone using MCRs
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Szardenings A.K., Antonenko V., Campbell D.A., DeFrancisco N., Ida S., Shi L., Sharkov N., Tien N., Wang Y., Navre M. Identification of highly selective inhibitors of collagenase-1 from combinatorial libraries of diketopiperazines. J Med Chem. 42:1999;1348-1357. The synthesis of nanomolar inhibitors of collagenase-I, with a high selectivity over gelatinase and stromelysine, is described with a diketopiperazine backbone using MCRs.
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(1999)
J Med Chem
, vol.42
, pp. 1348-1357
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Szardenings, A.K.1
Antonenko, V.2
Campbell, D.A.3
DeFrancisco, N.4
Ida, S.5
Shi, L.6
Sharkov, N.7
Tien, N.8
Wang, Y.9
Navre, M.10
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