Novel triethylsilane mediated reductive N-alkylation of amines:: improved synthesis of 1-(4-imidazolyl)methyl-4-sulfonylbenzodiazepines new farnesyltransferase inhibitors

被引：81

作者：

Chen, BC ^{[1
]}

Sundeen, JE ^{[1
]}

Guo, P ^{[1
]}

Bednarz, MS ^{[1
]}

Zhao, R ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Discovery Chem, Princeton, NJ 08543 USA

来源：

TETRAHEDRON LETTERS | 2001年 / 42卷 / 07期

关键词：

D O I：

10.1016/S0040-4039(00)02257-7

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An improved synthesis of 1-(imidazolyl)methyl-4-sulfonylbenzodiazapines, new farnesyltransferase inhibitors, was achieved using a novel reductive N-alkylation method. The new method involves reaction of a secondary amine with an aldehyde using triethylsilane in the presence of trifluoroacetic acid, giving a tertiary amine in 90-95% isolated yields. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1245 / 1246

页数：2

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