Department of Chemistry and Winship Cancer Institute , Emory University , Atlanta , Georgia 30322 , United States.
J Am Chem Soc. 2019 Mar 6;141(9):4147-4153. doi: 10.1021/jacs.9b01077. Epub 2019 Feb 21.
A mild, modular, and practical catalytic system for the synthesis of the highly privileged phenethylamine pharmacophore is reported. Using a unique combination of organic catalysts to promote the transfer of electrons and hydrogen atoms, this system performs direct hydroarylation of vinyl amine derivatives with a wide range of aryl halides (including aryl chlorides). This general and highly chemoselective protocol delivers a broad range of arylethylamine products with complete regiocontrol. The utility of this process is highlighted by its scalability and the modular synthesis of an array of bioactive small molecules.
报道了一种温和、模块化且实用的催化体系，用于合成高度特权的苯乙胺药效团。该体系使用独特的组合有机催化剂来促进电子和氢原子的转移，可实现乙烯基胺衍生物与各种芳基卤化物（包括芳基氯化物）的直接氢芳基化。该通用且高化学选择性的方案可提供具有完全区域选择性的广泛的芳基乙胺产物。该过程的实用性通过其可扩展性和一系列生物活性小分子的模块化合成得到了突出体现。
