苄胺与三氟甲基芳烃的α-二氟烷基化反应
α-Difluoroalkylation of Benzyl Amines with Trifluoromethylarenes.
作者信息
Yue Wen-Jun, Martin Ruben
机构信息
Institute of Chemical Research of Catalonia (ICIQ), The Barcelona Institute of Science and Technology, Av. Països Catalans 16, 43007, Tarragona, Spain.
Universitat Rovira i Virgili, Departament de Química Analítica i Química Orgànica, c/Marcel⋅lí Domingo, 1, 43007, Tarragona, Spain.
出版信息
Angew Chem Int Ed Engl. 2023 Oct 2;62(40):e202310304. doi: 10.1002/anie.202310304. Epub 2023 Aug 29.
An α-difluoroalkylation of benzyl amines with trifluoromethylarenes is disclosed herein. This protocol is characterized by its operational simplicity, excellent chemoselectivity and broad scope-even with advanced synthetic intermediates-, thus offering a new entry point to medicinally-relevant α-difluoroalkylated amines from simple, yet readily accessible, precursors.
本文公开了一种苄胺与三氟甲基芳烃的α-二氟烷基化反应。该方法的特点是操作简单、化学选择性优异且适用范围广泛——即使对于复杂的合成中间体也是如此——从而为从简单且易于获得的前体合成与药物相关的α-二氟烷基化胺提供了一个新的切入点。
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