School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan 430074, China.
J Org Chem. 2020 Aug 7;85(15):10143-10151. doi: 10.1021/acs.joc.0c01484. Epub 2020 Jul 27.
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.
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。
