Ugi reaction for the synthesis of 4-aminopiperidine-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil

被引:38
作者
Malaquin, Sandra
Jida, Mouhamad
Gesquiere, Jean-Claude
Deprez-Poulain, Rebecca
Deprez, Benoit [1 ]
Laconde, Guillaume
机构
[1] Univ Lille Nord France, Fac Pharm, INSERM, U761, F-59006 Lille, France
关键词
Ugi reaction; Remifentanil; Carfentanil; Mumm rearrangement; 4-COMPONENT CONDENSATION; AMINO-ACIDS; ISOCYANIDE;
D O I
10.1016/j.tetlet.2010.03.120
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A two-step sequence involving an Ugi four-component reaction was developed for the preparation of 4-acid derivatives. This strategy has led to the successful preparation of two carfentanil and remifentanil in shorter times and better yields than previously described methods. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2983 / 2985
页数:3
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