Design and Synthesis of TY-Phos and Application in Palladium-Catalyzed Enantioselective Fluoroarylation ofgem-Difluoroalkenes
Design and Synthesis of TY-Phos and Application in Palladium-Catalyzed Enantioselective Fluoroarylation ofgem-Difluoroalkenes
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TY-Phos的设计合成及其在钯催化宝石二氟烯烃对映选择性氟芳基化反应中的应用
DOI：
10.1002/anie.202008262
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发表时间：
2020-10-15
影响因子：
16.6
通讯作者：
Zhang, Junliang
中科院分区：
文献类型：
--
作者：
Lin, Tao-Yan;Pan, Zhangjin;Zhang, Junliang
首次报道了一种新型手性亚磺酰胺膦配体TY-Phos用于偕二氟烯烃与卤代芳烃的高对映选择性氟芳基化反应。N-Me-TY-Phos可以从容易获得的起始原料在三个步骤中以克规模容易地合成。本工作的显着特点，包括容易获得的起始原料，良好的产率，高的对映选择性以及广泛的底物范围，使这种方法非常实用和有吸引力。值得注意的是，还报道了生物活性分子类似物的不对称合成。
The first example of highly enantioselective fluoroarylation of gem-difluoroalkenes with aryl halides is presented by using a new chiral sulfinamide phosphine (Sadphos) type ligandTY-Phos. N-Me-TY-Phoscan be easily synthesized on a gram scale from readily available starting materials in three steps. Salient features of this work including readily available starting materials, good yields, high enantioselectivities as well as broad substrate scope make this approach very practical and attractive. Notably, the asymmetric synthesis of an analogue of a biologically active molecule is also reported.