State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, P.R. China.
Chemical Synthesis and Pollution Control Key Laboratory of Sichuan Province/College of Chemistry & Chemical Engineering, China West Normal University, Nanchong 637009, P.R. China.
Org Lett. 2020 Jul 17;22(14):5479-5485. doi: 10.1021/acs.orglett.0c01836. Epub 2020 Jun 30.
A palladium-catalyzed asymmetric allylation of -fluorenyl trifluoromethyl imine with allylic acetates is disclosed. This method provides scalable and efficient access to polysubstituted chiral α-trifluoromethyl amines bearing two adjacent stereocenters and one allyl group in high yields with excellent regio-, diastereo-, and enantioselectivity. Importantly, this method also provides a powerful strategy for the synthesis of both regioisomeric products and the regioselectivity is controlled by the chiral catalysts and optically active substrates.
本文报道了钯催化的 - 芴基三氟甲基亚胺与烯丙基乙酸酯的不对称烯丙基化反应。该方法提供了一种可扩展且高效的方法，以高收率和优异的区域选择性、非对映选择性和对映选择性，获得了带有两个相邻手性中心和一个烯丙基的多取代手性α-三氟甲基胺。重要的是，该方法还为两种区域异构体产物的合成提供了一种强大的策略，区域选择性由手性催化剂和光学活性底物控制。
