Rapid microwave-enhanced synthesis of 4-hydroxyquinolinones under solvent-free conditions

被引：65

作者：

Lange, JHM ^{[1
]}

Verveer, PC ^{[1
]}

Osnabrug, SJM ^{[1
]}

Visser, GM ^{[1
]}

机构：

[1] Solvay Pharmaceut, Res Labs, NL-1380 DA Weesp, Netherlands

来源：

TETRAHEDRON LETTERS | 2001年 / 42卷 / 07期

关键词：

anilides; MDL-104,653; microwave heating; quinolinones;

D O I：

10.1016/S0040-4039(00)02244-9

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

3-Aryl-4-hydroxyquinolin-2(1H)-ones are potent and selective glycine-site NMDA receptor antagonists of pharmaceutical interest. A novel microwave-enhanced synthesis of such quinolinones under solvent-free conditions has been developed. The quinolinones are easily obtained in a one-pot procedure as a result of the formal amidation of a malonic ester derivative with an aniline and subsequent cyclisation of the intermediate malondianilides. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1367 / 1369

页数：3

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