2-Substd. amino-thiazoline cpds. prodn. - by reaction of corresp. prim. amino cpd. with amine in presence of acid catalyst, useful as pharmaceutical intermediates

摘要

Prodn. of 2-substd. amino-thiazoline derivs. of formula (I) comprises reacting 2-amino-thiazoline (II) with amine R1R2NH (III) in presence of an acid catalyst. R1 and R2 = alkyl or alkenyl, opt. substd. phenyl or benzyl, or a heterocyclic gp., and one of them can also be H; R1 and R2 may together complete a heterocycle, opt. contg. additional heteroatoms. Pref. the catalyst is p-toluenesulphonic or methanesulphonic acids. The catalyst is 5-50 (pref. 15-40) mole % on (II), and the amine (III) is 2-30 (pref. 5-15) moles per mole (II). Reaction is at 100-200 (pref. 140-180)deg. C in an inert solvent, e.g. toluene, for 2-10 hrs.. USE/ADVANTAGE - (I) are intermediates for pharmaceuticals and other technical cpds.. This method is simple (single step) and provides good yields of high quality (I).