Design, Synthesis of TY-Phos and Application in Palladium-Catalyzed Enantioselective Fluoroarylation of gem-Difluoroalkenes.,Angewandte Chemie International Edition

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Design, Synthesis of TY-Phos and Application in Palladium-Catalyzed Enantioselective Fluoroarylation of gem-Difluoroalkenes.
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2020-09-06 , DOI: 10.1002/anie.202008262
Tao-Yan Lin _{1,

2} , Zhangjin Pan ₂ , Youshao Tu ₃ , Shuai Zhu ₂ , Hai-Hong Wu ₂ , Yu Liu ₃ , Zhiming Li ₁ , Junliang Zhang ₁

Affiliation

The first example of highly enantioselective fluoroarylation of gem‐difluoroalkenes with aryl halides is presented by using a new chiral sulfinamide phosphine (Sadphos) type ligand TY‐Phos. N‐Me‐TY‐Phos can 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.

中文翻译：

TY-Phos的设计，合成及其在钯催化的对二氟烯烃对映选择性氟芳基化反应中的应用。

通过使用新的手性亚磺酰胺膦（Sadphos）型配体TY-Phos，提出了使用芳基卤化物进行对二氟烯烃高对映选择性氟芳基化反应的第一个例子。N-Me- TY-Phos可以很容易地从克制的原料中分三步以克为单位合成。这项工作的显着特点包括容易获得的起始原料，良好的收率，高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。

更新日期：2020-09-06

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