The present disclosure relates to a novel, highly efficient and enantiospecific borylation method to synthesize a wide range of enantiopure alfa-amino tertiary boronic esters, and novel alfa-amino tertiary boronic acids and esters prepared by the method. More specifically, highly enantiospecific borylation of configurationally stable α-N-Boc substituted tertiary organolithium species and HBpin has been developed to synthesize various alfa-amino tertiary boronic esters through the formation of a new C—B bond with excellent enantiopurities.
本公开涉及一种新颖、高效且对映选择性
硼化方法,用于合成广泛范围的对映纯α-
氨基三级
硼酸酯,以及通过该方法制备的新型α-
氨基三级
硼酸和酯。更具体地说,通过高度对映选择性的
硼化方法,可以合成各种α-
氨基三级
硼酸酯,通过形成新的C—B键来获得优异的对映纯度,该方法涉及构型稳定的α-N-Boc取代的三级
有机锂物种和HBpin的
硼化。