Synthesis of C7-Functionalized Indoles through an Aromaticity Destruction–Reconstruction Process
Organic Letters(2022)
摘要
A process for the synthesis of C7-functionalized indoles using para-substituted 2-alkynylanilines as starting materials was reported. The process involves a dearomatization, an 1,2-addition by organic lithium or Grignard reagents, an aromatization-driven allylic rearrangement, and a cyclization. A variety of groups including alkyl, aryl, alkenyl, or alkynyl groups were selectively installed at the C7 site of indoles leading to the formation of 2,5,7-trisubstituted indoles.
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关键词
indoles,aromaticity destruction–reconstruction,synthesis
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