Convenient synthetic approach to 2,4-disubstituted quinazolines

被引：93

作者：

Ferrini, Serena

Ponticelli, Fabio

Taddei, Maurizio

机构：

[1] Univ Siena, Dipartimento Chim, I-53100 Siena, Italy

[2] Univ Siena, Dipartimento Farmacochim Tecnol, I-53100 Siena, Italy

来源：

ORGANIC LETTERS | 2007年 / 9卷 / 01期

关键词：

D O I：

10.1021/ol062540s

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

2,4-Dialkyl or aryl quinazolines have been prepared in three steps starting from easily available anilides. A photochemically induced Fries rearrangement of the anilides gave several ortho-aminoacylbenzene derivatives that were acylated at the NH2. These acylamides underwent rapid cyclization to 2,4-disubstituted quinazolines (and benzoquinazolines) in the presence of ammonium formate under microwave activation. This procedure is compatible with different functional groups and allowed also the preparation of new quinazolines derived from naturally occurring amino acids.

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页码：69 / 72

页数：4

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