K. El-Bayouki, W. Basyouni
Oct 1, 1988
Citations
0
Influential Citations
13
Citations
Journal
Bulletin of the Chemical Society of Japan
Abstract
Ethyl chloroformate/DMF mixture is used as a reagent for the facile ring closure of 5-amino-2-(ethylthio)thiazole-4-carboxamide (1a) to afford an excellent yield of 2-ethylthiothiazolo[5,4-d]pyrimidin-7(6H)-one (3). The action of phosphoryl chloride on the latter product gave its 7-chloro derivative (4). The corresponding 7-(dicyanomethyl) (5a), 7-[cyano(ethoxycarbonyl)methyl] (5b), and 7-(substituted amino)derivatives (6a–j) are synthesized from reactions of malononitrile, ethyl cyanoacetate, and primary amines, respectively, with compound 4. Most of the obtained products have been screened for activity against the intermediate host of schistosomiasis, B. alexandrina snails.