通过叠氮自由基加成和分子氧捕获进行吲哚的去芳构化反应以获得 2-叠氮吲哚啉-3-醇。
Dearomatization of Indoles via Azido Radical Addition and Dioxygen Trapping To Access 2-Azidoindolin-3-ols.
出版信息
Org Lett. 2019 Aug 16;21(16):6217-6220. doi: 10.1021/acs.orglett.9b02009. Epub 2019 Jul 30.
PMID:31361144
Abstract
Efficient copper-catalyzed aerobic oxidative dearomatization of indoles with trimethylsilyl azide (TMSN) for the synthesis of 2-azidoindolin-3-ols has been developed. Molecular oxygen served as the oxygen-atom source in this transformation. The multicomponent reaction is appreciated by its high site- and diastereoselectivity, broad substrate scope, and mild conditions at room temperature.
摘要
已开发出一种高效的铜催化有氧氧化吲哚与三甲基硅基叠氮（TMSN）的去芳构化反应，用于合成 2-叠氮吲哚啉-3-醇。在这种转化中，分子氧作为氧原子源。该多组分反应具有高的位点和非对映选择性、广泛的底物范围以及在室温下温和的条件等优点，受到了人们的赞赏。
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