One aspect of the present invention relates to methods of asymmetric synthesis, e.g., asymmetric hydride reductions of carbonyl groups, using a chiral, non-racemic phase transfer catalyst, a helper nucleophile, and a sterically bulky reagent nucleophile, e.g., an alkoxyhydride derived from a sacrificial ketone and a hydride reagent. Moreover, the sterically bulky reagent nucleophile may be generated in situ or prepared in a prior step. Another aspect of the present invention relates to chiral non-racemic phase transfer catalysts, and their use in the subject methods.
本发明的一个方面涉及不对称合成的方法,例如,羰基的不对称
氢化物还原,使用手性、非消旋相转移催化剂、辅助亲核剂和立体笨重的试剂亲核剂,例如,由牺牲酮和
氢化物试剂衍生的烷氧基酸酐。此外,立体笨重的试剂亲核体可以在原位生成,也可以在之前的步骤中制备。本发明的另一方面涉及手性非外消旋相转移催化剂及其在主题方法中的使用。