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光学活性的2-羟甲基-3-芳基丙酸类化合物是许多手性药物的关键合成中间体,但到目前为止其不对称合成方法大多存在对映选择性不高及/或底物范围有限等问题.报道了手性SpinPHOX/Ir(I)络合物在一系列2-羟甲基-3-芳基丙烯酸的不对称氢化中表现出优良的催化性能,取得完全的底物转化和良好到优秀的对映选择性(高达95%ee).对于同一2-羟甲基-3-芳基丙烯酸底物的不对称氢化,使用中心手性相同但螺环骨架上的轴手性相反的催化剂分别以优良的对映选择性获得构型相反的产物,从而为光学活性2-羟甲基-3-芳基丙酸及相关手性药物的不对称合成提供了一条简便高效的途径.
Optically active 2-hydroxymethyl-3-arylpropionic acid compounds are key synthetic intermediates for many chiral drugs, but to date most of their asymmetric synthesis methods have enantioselectivity and / or substrate Limited range etc. It was reported that the chiral SpinPHOX / Ir (I) complex showed excellent catalytic performance in the asymmetric hydrogenation of a series of 2-hydroxymethyl-3-arylacrylic acid and achieved complete substrate conversion And good to excellent enantioselectivity (up to 95% ee). For the asymmetric hydrogenation of the same 2-hydroxymethyl-3-arylacrylic acid substrate, using a chiral center of the same chirality but with a spherocyclic backbone The opposite catalyst, respectively, with an excellent enantioselectivity to obtain the oppositely configured product provides an efficient and convenient route for the asymmetric synthesis of optically active 2-hydroxymethyl-3-arylpropionic acid and related chiral drugs .