Synthetic strategies for piperazine derivatives

作     者：翟亚亚 闫钢 黄文杰 牛彦 许凤荣 梁磊 王超 徐萍 

作者机构：北京大学医学部药学院药物化学系北京100191 

基　　金：National Basic Research Program of China(Grant No.2012CB518000) the National Natural Science Foundation of China(Grant No.21172012) the Specialized Research Fund for the Doctoral Program of Higher Education of China(Grant No.20120001110010) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2014年第23卷第8期

页      码：572-577页

摘      要：As important constitutes in many drugs, piperazine comprised compounds are of great interest for drug design. In this paper, two piperazine-based compounds were synthesized for the first time, with different strategies exploited. For one compound, a highly reactive intermediate of isothiocyanate was constructed to get the desired piperazinecarbothioamide. The synthesis of the other compound was completed sequentially through Friedel-Crafts acylation, coupling reaction and Michael addition. Both synthetic routes have short steps and acceptable yields, and such strategies can be applied to the synthesis of similar oioerazine-containin~ comoounds.

主 题 词：Piperazine Synthesis strategy Isothiocyanate Michael addition Friedel-Crafts acylation 

学科分类：1007[医学-药学类] 100701[100701] 10[医学] 

核心收录：

D　O　I：10.5246/jcps.2014.08.074

馆 藏 号：203131982...