摘要
We report herein the first example of asymmetric hydroazidation of α-substituted vinyl ketones by using chiral primary amines as the catalysts.A simple chiral primary-tertiary diamine catalyst derived from lphenylalanine was found to readily promote this aza-Michael addition reaction with enamine protonation as the key stereogenic step,thus enabling the effective synthesis of α-chiral β-azido ketones with good yields and moderate enantioselectivities.
We report herein the first example of asymmetric hydroazidation of α-substituted vinyl ketones by using chiral primary amines as the catalysts.A simple chiral primary-tertiary diamine catalyst derived from lphenylalanine was found to readily promote this aza-Michael addition reaction with enamine protonation as the key stereogenic step,thus enabling the effective synthesis of α-chiral β-azido ketones with good yields and moderate enantioselectivities.
基金
National Natural Science Foundation of China(NSFC Nos.21390400,21521002 and 21502198)
the Ministry of Science and Technology,Chinese Academy of Sciences(No.QYZDJSSW-SLH023)for generous financial support
supported by National Program for Support of Top-notch Young Professionals,CAS Youth Innovation Promotion Association and CAS onehundred talented program(D)
