Soluble polymer-supported synthesis of arylpiperazines

被引：39
|
作者：
Pan, PC [1 ]
Sun, CM [1 ]
机构：
[1] Natl Dong Hwa Univ, Dept Chem, Hualien 974, Taiwan
来源：
TETRAHEDRON LETTERS | 1998年 / 39卷 / 51期
关键词：
alkylation; acylation; piperazine; solid-phase synthesis;
D O I：
10.1016/S0040-4039(98)02224-2
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A method for soluble. inexpensive polymer-supported synthesis of piperazine and piperidine libraries on the basis of nucleophilic aryl substitution (SNAr) and N-acylation is reported. Asymmetric N, N'-disubstituted piperazine and piperidine derivatives, that are potential drug candidates, can be synthesized in quantitative yields and excellent purity after several steps by simple precipitation and washing. This liquid phase method should prove to be a useful tool for constructing combinatorial libraries containing diamine moiety. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：9505 / 9508
页数：4
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