A concise route to triazolobenzodiazepine derivatives via a one-pot alkyne-azide cycloaddition reaction

被引：47

作者：

Thomas, AW ^{[1
]}

机构：

[1] F Hoffmann La Roche & Cie AG, Div Pharmaceut, Discovery Chem, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(02)00262-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new and efficient one-pot synthesis of [1,2,3]triazolo[1,5-a][1,4] benzodiazepin-6(4H)-ones is described starting from readily available anthranilic acids. A small array of the title compounds were assembled via a four-step sequence involving diazotisation, azide addition followed by amide bond formation employing polymer supported carbodiimide and subsequent 1,3-dipolar cycloaddition reaction. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1881 / 1884

页数：4

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