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环境友好型吲哚衍生物的 2,3-二官能化方法。

Environmentally Friendly Protocol for 2,3-Difunctionlization of Indole Derivatives.

机构信息

School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan 430074, China.

出版信息

J Org Chem. 2020 Aug 7;85(15):10143-10151. doi: 10.1021/acs.joc.0c01484. Epub 2020 Jul 27.

Abstract

Environmentally friendly and highly regioselective C-3 dichlorination and C-2 oxidation of N-substituted indoles have been established using NaCl as a chlorine source and HO as an oxygen source. A series of 3,3-dichloro-2-oxindoles were obtained in moderate to excellent yields. The gram-scale synthesis and derivatization reaction were explored. The possible mechanism for this reaction was elucidated.

摘要

采用 NaCl 作为氯源,H 2 O 2 作为氧源,建立了一种环境友好、高区域选择性的 N-取代吲哚的 C-3 二氯化和 C-2 氧化方法。以中等至优秀的收率得到了一系列 3,3-二氯-2-氧吲哚。探讨了克级合成和衍生化反应。阐明了该反应的可能机理。

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