Solid phase synthesis of cyanoacetamidines: Fast access to potential bioisosteres of acceptor-substituted guanidines

被引：17

作者：

Zaragoza, F

机构：

[1] Novo Nordisk A/S, DK-2760 Måløv, Novo Nordisk Park

来源：

TETRAHEDRON LETTERS | 1997年 / 38卷 / 41期

关键词：

D O I：

10.1016/S0040-4039(97)01694-8

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A synthesis of cyanoacetamidines has been developed, which can be realized on solid support. Reaction of resin-bound cyanoacetic acid with aromatic isothiocyanates yielded thioamides, which could be condensed with primary or secondary aliphatic or aromatic amines in the presence of EDC to yield ketene aminals, TFA-mediated cleavage from the support with concomitant decarboxylation gave cyanoacetamidine trifluoroacetates in purities up to 83% (HPLC, 254 nm). (C) 1997 Elsevier Science Ltd.

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页码：7291 / 7294

页数：4

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