Catalytic Strategy for Regioselective Arylethylamine Synthesis
Catalytic Strategy for Regioselective Arylethylamine Synthesis
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DOI：
10.1021/jacs.9b01077
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发表时间：
2019-03-06
影响因子：
15
通讯作者：
Jui, Nathan T.
中科院分区：
文献类型：
--
作者：
Boyington, Allyson J.;Seath, Ciaran P.;Jui, Nathan T.
报道了一种温和的、模块化的、实用的用于合成高度特权的苯乙胺药效团的催化体系。使用有机催化剂的独特组合来促进电子和氢原子的转移，该系统用广泛的芳基卤化物（包括芳基氯化物）进行乙烯胺衍生物的直接氢化芳基化。这种通用和高度化学选择性的协议提供了广泛的芳基乙胺产品与完整的区域控制。该过程的实用性突出了其可扩展性和生物活性小分子阵列的模块化合成。
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.