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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… Click to show full abstract
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.
Keywords:
synthesis functionalized;
functionalized indoles;
indoles aromaticity;
process synthesis;
aromaticity destruction
Journal Title: Organic letters
Year Published: 2022
Link to full text (if available)
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Journal Title: Organic letters
Year Published: 2022
Link to full text (if available)
Share on Social Media: Sign Up to like & get
recommendations!