Soluble polymer-supported synthesis of arylpiperazines

A method for soluble. inexpensive polymer-supported synthesis of piperazine and piperidine libraries on the basis of nucleophilic aryl substitution (S NAr) and N-acylation is reported. Asymmetric N, N'-disubstituted piperazine and piperidine derivatives, that are potential drug candidates, can be syn thesized 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 diami ne moiety. (C) 1998 Elsevier Science Ltd. All rights reserved.