Synthesis of (R)-Bufuralol

Abstract

Bufuralol is a non-selective β-adrenoceptor blocker comparable to propanol-ol in potency. It is also a β-adrenergic receptor antagonist and an inhibitor of testosterone 6β-hydroxylase. The key step in the synthesis depicted is the dynamic kinetic resolution of racemic chlorohydrin F using racemization catalyst G together with selective esterification of the (R)-chlorohydrin F by lipase PS-C Amano II and isopropenyl acetate.