环胺类联二萘酚配体对催化炔烃与芳基麟酰亚胺加成反应初探

BINOL-Cycloamine ligands catalytic asymmetric addition of alkynes to N-diphenylphosphonimide

本文发展了一种新的简便的方法,用于制备系列含环胺类骨架联二萘酚(BINOL-Cycloamine)配体。此类配体联合Et_(2)Zn可用于催化端基炔对N-二苯基膦酰亚胺的不对称加成反应,合成炔丙基胺类产物。其中筛选出的配体有效催化合成炔丙基胺类产物,产率高达85%,对映选择性ee值57%。

A new and convenient method for the preparation of a series of optically active BINOL-Cycloamine ligands had been developed.These ligands in combination with ZnEt_(2) were used to catalyze the reaction of N-(diphenylphosphinoyl)imines with terminal alkynes for the asymmetric synthesis of propargylic amines.One of the ligands was found to exhibit good yield(85%)and promising enantioselectivity(57%ee).