Efficient synthesis of 1-heterocyclic-3-aminopyrrolidinones

被引:22
作者
Bell, IM [1 ]
Beshore, DC [1 ]
Gallicchio, SN [1 ]
Williams, TM [1 ]
机构
[1] Merck & Co Inc, Dept Med Chem, Merck Res Labs, W Point, PA 19486 USA
关键词
3-aminopyrrolidinones; nitrogen heterocycles; Mitsunobu reaction; cyclization;
D O I
10.1016/S0040-4039(99)02282-0
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A novel two-step synthesis of optically active 3-aminopyrrolidinones is described. The route allows access to pyrrolidinones with heterocyclic functionality that is incompatible with known methodology, and affords the final products in good to excellent yield and high enantiomeric purity. The Mitsunobu cyclodehydration is shown to be an efficient method for the formation of a variety of gamma-lactams. (C) 2000 Published by Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1141 / 1145
页数:5
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