Gold-Catalyzed Cascade Reaction of 2-Alkynyl Aryl Azides with Enecarbamates for Direct Synthesis of α-(3-Indolyl)ketones

作者:Xie, Jin-Ming; Zhu, Yun-Long; Fu, Yan-Ming; Zhu, Cheng-Feng; Cheng, Lan-Jun; You, Yang-En; Wu, Xiang*; Li, You-Gui
来源:Organic Letters, 2023, 25(2): 421-425.
DOI:10.1021/acs.orglett.2c04147

摘要

alpha-(3-Indolyl)ketones are essential building blocks for the generation of biologically active molecules. We described a new method for the direct assembly of alpha-(3-indolyl)ketones through the cascade reaction of 2-alkynyl aryl azides with enecarbamates, in which the in situ generated alpha-imino gold carbene intermediate was trapped by enecarbamate to achieve umpolung reactivity of indole at the 3-position.