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Angew.Chem.Int.Ed.2015,54,2260~2264手性γ-仲胺基醇作为(S)-度洛西汀、(R)-氟西汀以及(R)-阿托莫西汀等重要药物的关键中间体,其不对称合成方法的研究一直备受关注.其中不对称催化氢化β-仲胺基酮的方法被认为是最具经济性的路线,但是至今为止相关研究报道寥寥无几.其原因在于底物的特殊性使得该反应对催化体系的要求非常高.催化体系不但需要实现优秀的对映选择性,同时还要保证很高的催化活性以降低原料变质引起的副反应.上海交通大学化学化工学院张万斌课题组利用氯化锌辅助的磷手性双膦-铑配合物催化体系,成功地实现了β-仲胺基酮的高效不对称催化氢化.合成的手性γ-
Angew. Chem. Int. Ed. 2015, 54, 2260-2264 Chiral γ-secondary aminoalcohols as (S) -dexulothine, (R) -fluoxetine and (R) And other key intermediates of important drugs, the asymmetric synthesis of research methods have been of great concern.Among them asymmetric catalytic hydrogenation of β-secondary amine ketone is considered the most economical route, but so far so few related studies reported Due to the special nature of the substrate makes the reaction of the catalyst system is very high.Catalyst system not only need to achieve excellent enantioselectivity, but also to ensure high catalytic activity to reduce side effects caused by deterioration of raw materials Shanghai Jiaotong University School of Chemistry and Chemical Engineering Zhang Wanbin group using zinc chloride-assisted phosphorus chiral biphosphine-rhodium complex catalytic system, the successful realization of β-secondary amino ketone efficient asymmetric catalytic hydrogenation of synthetic chiral γ -