Short synthesis of protease inhibitors via modified Passerini condensation of N-Boc-α-aminoaldehydes

被引:65
作者
Banfi, L [1 ]
Guanti, G [1 ]
Riva, R [1 ]
Basso, A [1 ]
Calcagno, E [1 ]
机构
[1] Dipartimento Chim & Chim Ind, I-16146 Genoa, Italy
关键词
Passerini reaction; protease inhibitors; peptidomimetic; multicomponent reactions; isocyanicles; oxoamides;
D O I
10.1016/S0040-4039(02)00728-1
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Extension of the previously reported modification of Passerini multicomponent reaction (involving condensation with N-Boc-alpha-aminoaldehydes followed by a deprotection-transacylation step) to alpha-aminoacid derived carboxylic or isocyanide components, allowed the highly convergent and short synthesis of complex peptidomimetic structures, including known potent inhibitors of serine proteases. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:4067 / 4069
页数:3
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