Department of Chemistry , Zhejiang University , Hangzhou 310027 , China.
Department of Chemistry , Zhejiang Sci-Tech University , Hangzhou 310018 , China.
J Org Chem. 2019 Oct 18;84(20):13013-13021. doi: 10.1021/acs.joc.9b01815. Epub 2019 Sep 6.
A rhodium-catalyzed redox-neutral reaction of arylhydrazines with sulfoxonium ylides to construct 2-arylindole derivatives in one pot has been developed. The transformation proceeds efficiently under mild conditions and involves tandem C-H activation and an intramolecular dehydration annulation sequence, providing a straightforward pathway to access pharmaceutically and biologically valuable 1-aminoindole derivatives.
发展了一种铑催化的芳基腙与亚砜叶立德的氧化还原中性反应,一锅法构建 2-芳基吲哚衍生物。该转化在温和条件下高效进行,涉及串联的 C-H 活化和分子内脱水环合反应序列,为获得具有药用和生物价值的 1-氨基吲哚衍生物提供了一条直接途径。