Novel and general method for the preparation of peptidyl argininals

被引:28
作者
Tamura, SY
Semple, JE
Ardecky, RJ
Leon, P
Carpenter, SH
Yu, G
Shamblin, BM
Weinhouse, MI
Ripka, WC
Nutt, RF
机构
[1] Corvas International, Inc., San Diego, CA 92121
关键词
D O I
10.1016/0040-4039(96)00777-0
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A general method for the synthesis of peptidyl argininals was developed which utilizes the novel building block N-g-nitro-L-argininal ethyl aminal . HCl. The final aldehyde structure is generated by hydrolysis of the peptidic aminal moiety and can be applied to highly functionalized peptidic structures. The method is amenable to the preparation of large quantities of enantiomerically pure peptidyl argininals and was applied to the synthesis of two potent thrombin inhibitors. (C) 1996 Elsevier Science Ltd
引用
收藏
页码:4109 / 4112
页数:4
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