不对称硼烷还原合成手性氨基醇  

Synthesis of Chiral Amino Alcohols by Enantioselective Borane Reduction

作　　者：沈宗旋[1] 李咏华[1] 秦宏兵[1] 张雅文[1] 

机构地区：[1]苏州大学化学化工学院江苏省有机合成重点实验室,江苏苏州215006

出　　处：《化学研究》2004年第3期23-26,49,共5页Chemical Research

摘　　要：用原位生成的手性噁唑硼烷为催化剂,用2molBH3对1molα 或β 氨基酮进行了对映选择性还原,生成光学活性氨基醇 硼烷络合物,后者脱去BH3后给出光学活性氨基醇,ee值最高达99%.讨论了氨基酮结构与反应选择性的关系.A group of α- and β- dialkylaminoketones were reduced enantioselectively by using BH_3-THF and the in-situ formed chiral oxazaborolidine.The formed optically active aminoalcohol-borane complexes, which, after deboration gave optically active aminoalcohols with the ee up to 99%. The effects of the substrate structure on the enantioselectivity of the reaction were discussed.

关 键 词：硼烷 合成 手性氨基醇 对映选择性还原 氨基酮 手性药物 

分 类 号：TQ463.26[化学工程—制药化工]