Alkylation/Ipso-cyclization of Active Alkynes Leading to 3-Alkylated Aza- and Oxa-spiro[4,5]-trienones

J Org Chem. 2022 May 6;87(9):5643-5659. doi: 10.1021/acs.joc.1c03118. Epub 2022 Apr 13.

Abstract

A method for the preparation of 3-alkylated spiro[4.5]trienones via alkylation/ipso-cyclization of activated alkynes with 4-alkyl-DHPs under transition-metal-free conditions is proposed. This alkylation successively undergoes the generation of alkyl radicals, addition of alkyl radicals to the alkynes, and intramolecular ipso-cyclization. The mechanism studies suggest that the alkylation/ipso-cyclization involves a radical process. This ipso-cyclization procedure shows a series of advantages, such as accessibility, mild conditions, high efficiency, greater safety, and an environmentally friendly method.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Alkynes*
  • Cyclization
  • Spiro Compounds*

Substances

  • Alkynes
  • Spiro Compounds