New Amidoesters of P(III) Acids on the Basis of 2-Amino-4-phenylthiazole

Abstract

Thiazole and its derivatives are the most important synthons for preparing various biologically active compounds. In detail, heterocyclic sulfanylamide derivatives include norsulfazol (2-sulfanylamidothiazole), a widely known antimicrobial sulfanylamide drug. With the purpose of searching for and synthesizing new medicines, we carried out purposeful chemical modification of 2-amino-4-phenylthiazole (I) to ÄÄÄÄÄÄÄÄÄÄÄÄ obtain new P(III) amidoesters. Starting thiazole I was prepared by the procedure in [1]. The reaction was carried out by heating equimolar amounts of thiazole I and tert-butyl tetraethylphosphorodiamidite (II) in ethyl acetate with simultaneous distillation of the evolving diethylamine (identified as hydrochloride). Reaction progress was controlled by TLC. Completion of the reaction was judged about by the amount of the hydrochloride obtained.