Synthesis of tricyclic 4-chloro-pyrimido[4,5-b][1,4]benzodiazepines

被引：65

作者：

Yang, JX ^{[1
]}

Che, X ^{[1
]}

Dang, Q ^{[1
]}

Wei, ZL ^{[1
]}

Gao, S ^{[1
]}

Bai, X ^{[1
]}

机构：

[1] Jilin Univ, Ctr Combinatorial Chem & Drug Discovery, Changchun 130012, Jilin, Peoples R China

来源：

ORGANIC LETTERS | 2005年 / 7卷 / 08期

关键词：

D O I：

10.1021/ol050181f

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] A novel methodology was developed for the efficient synthesis of 4-chloro-pyrimido[4,5-b][1,4]benzodiazepines. The key is the intramolecular Friedel-Crafts cyclization of 5-amino-4-(N-substituted)anilino-6-chloropyrimidine with either a carboxylic acid or its derivatives to construct the 4-chloro-pyrimido[4,5-b][1,4]benzodiazepine core. Subsequent nucleophilic substitution allows the introduction of one more diversity point in the target molecules. This strategy provides an efficient method to access a library of compounds based on privileged substructures that are of great interest in drug discovery.

引用

页码：1541 / 1543

页数：3

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