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由(1R,2S)-麻黄碱制得了五个新的手性硼杂(口恶)唑烷1~5,它们催化甲硼烷不对称还原苯乙酮,获得了高产率的具有38.5~72.4%e.e.的R-1-苯基乙醇。讨论了催化剂的结构-活性关系及反应参数(催化剂用量、反应温度)对还原反应对映选择性的影响。
Five new chiral boronic acid oxazolidines 1 ~ 5 were prepared from (1R, 2S) -ephedrine and they catalyzed the asymmetric reduction of acetophenone by borane. High yields were obtained with 38.5 ~ 72.4 % Ee of R-1-phenylethanol. The structure-activity relationship and the influence of reaction parameters (catalyst amount and reaction temperature) on the enantioselectivity of the reduction reaction were discussed.