Prepn. of new propranolol analogues - by reacting racemic oxirane(s) with optically active amine(s), then selective oxidn., useful in regulation of blood pressure

摘要

Prepn. of enriched diastereomers of propanolol analogues with two chiral centres, of formula (I) comprises (a) reaction of racemic oxiranes of formula (II) with optically active amines of formula (III); and (b) selective extn. of the resultant propanolol analogues (as their acid addn. salts) to give the enriched diastereomers. Ar = naphthyl, 4- or 6-methylnaphthyl, phenyl, 4-nitrophenyl, 2- or 4-chlorophenyl, tolyl or ureidophenyl; R1, R2 = 1-6C alkyl, opt. substd. phenyl, naphthyl or substd. benzyl; provided that R1 and R2 are different. USE/ADVANTAGE - (I) are regulators of blood pressure. The process is simple and involves few reaction steps.