Efficient Room-Temperature One-Pot Synthesis of 2-Amino-3-alkyl(3-aryl)quinazolin-4(3H)-ones

被引：14

作者：

Lecoutey, Cedric ^{[1
]}

Fossey, Christine ^{[1
]}

Rault, Sylvain ^{[1
]}

Fabis, Frederic ^{[1
]}

机构：

[1] Univ Caen Basse Normandie, Ctr Etud & Rech Medicament Normandie, UPRES EA 4258, UFR Sci Pharmaceut,INC3M FR CNRS 3038, F-14032 Caen, France

来源：

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY | 2011年 / 2011卷 / 15期

关键词：

Heterocycles; Fused-ring systems; Amination; Thioureas; Guanidines; SOLID-PHASE SYNTHESIS; THYMIDYLATE SYNTHASE; FACILE SYNTHESIS; INHIBITORS; QUINAZOLINES; DERIVATIVES; DISCOVERY; CONCISE; DESIGN;

D O I：

10.1002/ejoc.201100200

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Starting from anthranilates, the one-pot successive addition of ethoxycarbonylisothiocyanate, alkyl- or arylamines, and the coupling reagent EDCI led to the clean, room-temperature formation of carbamate-protected 2-amino-3-alkyl(3-aryl)quinazolin-4(3H)-ones in up to 93% yield. This method provides a practical alternative to previously reported procedures for the synthesis of 2-amino-3-substituted quinazolin-4(3H)-ones.

引用

页码：2785 / 2788

页数：4

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