二氟卡宾参与下从邻乙烯基苯胺出发构建3-取代吲哚酮类化合物

Difluorocarbene-Enabled Synthesis of 3-Substituted-2-oxoindoles from o-Vinylanilines

开发了一种新型的无需过渡金属参与的合成1-烷基-3-(2-氧代-2-芳基/烷基-乙基)吲哚酮的方法.这项工作揭示了氧吲哚骨架可以直接由邻乙烯基苯胺和市售的卤代二氟烷基试剂通过C—N裂解/新C—N键和C—C键形成来构建.该反应具有高效和优异的官能团兼容性,在药物分子和天然产物的后期修饰中具有巨大潜力.

A novel transition-metal-free protocol for the synthesis of 1-alkyl-3-(2-oxo-2-aryl/alkyl-ethyl)indolin-2-ones is developed.This work reveals that oxoindole skeletons can be directly constructed from ortho-vinylanilines and commercially available halogenated difluoroalkyl reagents via a C—N cleavage/new C—N bonds and C—C bond formation cascade.This reaction portrays high efficiency and excellent functional group compatibility,and has great potential in the late-stage modifications of pharmaceutical molecules and natural products.