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.
Org Lett. 2022 Jul 22;24(28):5109-5114. doi: 10.1021/acs.orglett.2c01941. Epub 2022 Jul 10.
Herein, we report a modular catalytic technique that streamlines the preparation of -difluoroalkanes from unactivated precursors. The method is characterized by its simplicity, generality, and site selectivity, including the functionalization of advanced intermediates and olefin feedstocks. Our approach is enabled by a cooperative interplay of halogen- and hydrogen-atom transfer, thus offering a new entry point to difluorinated alkyl bioisosteres of interest in drug discovery.
在此，我们报告了一种模块化的催化技术，可简化从非活化前体制备 -二氟烷烃的过程。该方法的特点是简单、通用和位点选择性，包括对高级中间体和烯烃原料的功能化。我们的方法得益于卤原子和氢原子转移的协同作用，从而为药物发现中感兴趣的二氟烷基生物等排体提供了一个新的切入点。
