Effects of Methyl Substituents on the Activity and Enantioselectivity of Homobenzotetramisole-Based Catalysts in the Kinetic Resolution of Alcohols

摘要

Substitution of the tetrahydropyrimidine ring in enantioselective acyl transfer catalyst homobenzotetramisole (HBTM) >6 with methyl groups exerts a dramatic influence on its performance in the kinetic resolution of secondary alcohols. Syn-3-Methyl analogue of HBTM (>9a) has proved to be superior to the parent compound in terms of catalytic activity, enantioselectivity, and synthetic accessibility.