Synthesis of Substituted Aminopyrimidines as Novel Promising Tyrosine Kinase Inhibitors

Abstract

A procedure has been proposed for the synthesis of a series of substituted N-(1,3-thiazol-2-yl)-pyrimidin-2-amines and N-(pyrimidin-2-yl)thioureas by reactions of diethyl 2-(ethoxymethylidene)malonate and ethyl 2-(ethyoxymethylidene)-3-oxobutanoate with 1,3-thiazol-2-ylguanidines and amidinothiourea, respectively. Preliminary screening has revealed high inhibitory activity of ethyl 2-(carbamothioylamino)-4-methylpyrimidine-5-carboxylate and ethyl 2-(carbamothioylamino)-6-oxo-1,6-dihydropyrimidine-5-carbox-ylate toward several protein kinases.