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以2-羟基蒎烷-3酮(2)为手性助剂,与2-氨甲基吡啶(3)缩合得到中间体酮亚胺4,经去质子化、不对称烷基化、转胺反应得到光学活性α-取代(2-吡啶基)甲胺(1),对映体过量值为89—98%.并提出了过渡态模型,对对映选择性合成反应作了较为合理的解释.
Hydroxyapinane-3-one (2) was used as a chiral auxiliary and was condensed with 2-aminomethylpyridine (3) to obtain the intermediate ketimine 4. After deprotonation, asymmetric alkylation, transamination The optically active α-substituted (2-pyridyl) methylamine (1) was obtained with an enantiomeric excess of 89-98%, and a transition state model was proposed to give a more reasonable explanation of the enantioselective synthesis reaction .