Traceless synthesis of 3H-quinazolin-4-ones via a combination of solid-phase and solution methodologies

被引：19

作者：

O'Mahony, DJR ^{[1
]}

Krchnák, V ^{[1
]}

机构：

[1] SIDDCO Inc, Tucson, AZ 85747 USA

来源：

TETRAHEDRON LETTERS | 2002年 / 43卷 / 06期

关键词：

D O I：

10.1016/S0040-4039(01)02268-7

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A solid-phase traceless synthesis of quinazolin-4-ones is described. An aldehyde functionalized resin was reductively aminated with primary amines, and the resin-bound secondary amine acylated with o-nitro-benzoic acids. The nitro group was reduced with tin(II) chloride, and the aniline acylated with acid anhydrides. Acidolytic cleavage afforded a diamide, which was cyclized in Solution phase to the 3H-quinazolin-4-one removing the trace of the linker. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：939 / 942

页数：4

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