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钯催化吲哚取代的烯丙基芳基卤化物与炔烃的 C-H 功能化反应构建吲哚生物碱骨架。

Pd-Catalyzed C-H Functionalization of Indole-Containing Alkene-Tethered Aryl Halides with Alkynes To Construct Indole Alkaloid Scaffolds.

机构信息

Inner Mongolia Key Laboratory of Fine Organic Synthesis, Department of Chemistry and Chemical Engineering, Inner Mongolia University, Hohhot 010021, China.

出版信息

Org Lett. 2022 Apr 22;24(15):2910-2914. doi: 10.1021/acs.orglett.2c00882. Epub 2022 Apr 8.

Abstract

A convenient and straightforward approach for the construction of indole alkaloid scaffolds from indole-containing alkene-tethered aryl halides and alkynes through a sequential C-H activation, five-membered palladacycle formation, and alkyne insertion process has been described. The approach provides a series of indole alkaloid compounds in moderate to excellent yields with good functional tolerance.

摘要

一种方便直接的方法,可通过顺序 C-H 活化、五元钯环形成和炔烃插入过程,从含吲哚的烯丙基芳基卤化物和炔烃构建吲哚生物碱支架。该方法以中等到优异的产率提供了一系列吲哚生物碱化合物,具有良好的功能耐受性。

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