Shanghai Key Laboratory of Green Chemistry and Chemical Processes, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, 200062, P.R. China.
Angew Chem Int Ed Engl. 2016 Oct 10;55(42):13316-13320. doi: 10.1002/anie.201607918.
A novel phosphine-catalyzed, highly enantioselective umpolung addition of trifluoromethyl ketimines to Morita-Baylis-Hillman carbonates was developed and it provides facile access to optically active trifluoromethyl amines with a chiral tertiary stereocenter under mild reaction conditions. The salient features of this reaction include general substrate scope, mild reaction conditions, good yields, high enantioselectivity, ease of scale-up to gram scale, and further transformations of the products.
发展了一种新型膦催化的、高对映选择性的三氟甲基亚胺到 Morita-Baylis-Hillman 碳酸酯的反转加成反应，在温和的反应条件下，提供了一种简便的方法来获得具有手性叔立体中心的光学活性的三氟甲基胺。该反应的显著特点包括广泛的底物范围、温和的反应条件、良好的产率、高对映选择性、易于放大到克级规模以及产物的进一步转化。
