Catalytic enantioselective Reformatsky reaction with ketonesf

摘要

Chiral tertiary alcohols were obtained with good yields and enantioselectivities via a catalytic Reformatsky reaction with ketones, including the challenging diaryl ketones, using chiral BINOL derivatives. Chiral tertiary alcohols are important structural units present in many biologically active compounds and pharmaceutical intermediates. An important strategy for the construction of this moiety is the catalytic enantioselective addition of carbon nucleophiles to ketones. However, this approach is difficult due to the lower reactivity of ketones and the decreased steric discrimination compared to aldehydes. Very few examples have been reported describing catalytic enantioselective aldol reactions to ketones.