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A general method for the solid-phase synthesis of unsymmetrical tri- and tetrasubstituted ureas
Changsheng Zheng1, Andrew P Combs
1Chemical and Physical Sciences, DuPont Pharmaceuticals Company, Experimental Station, P.O. Box 80500, Wilmington, Delaware 19880-0500, USA. changsheng.zheng@dupontpharma.com
Journal of Combinatorial Chemistry
|February 8, 2002
Abstract:
A general method for the preparation of unsymmetrical di, tri-, and tetrasubstituted ureas on polymer supports is presented. Polymer-bound primary and secondary amines react with imidazolium salts (urea donors), which are generated from the reaction of N,N'-carbonyldiimidazole (CDI) with primary and secondary amines followed by alkylation with MeI to give tri- and tetrasubstituted ureas in excellent yields (76-98%) and purities (80-99%).