Synthesis of dibenzocyclohepten-5-ones by electrophilic iodocyclization of 1-([1,1'-biphenyl]-2-yl)alkynones

J Org Chem. 2014 Apr 18;79(8):3452-64. doi: 10.1021/jo5001803. Epub 2014 Mar 31.

Abstract

A synthesis of iodo-substituted dibenzocyclohepten-5-ones by the iodine monochloride (or iodine)-induced intramolecular 7-endo-dig cyclization of 1-([1,1'-biphenyl]-2-yl)alkynones is reported. Detailed investigations on the substituent effects during the electrophilic iodocyclization of the alkynones show that they play a crucial role in determining the reaction pathways of the cyclization. By modifying the substitution pattern on the alkynone substrates, the cyclization takes place regioselectively, leading to either dibenzocyclohepten-5-ones, via a 7-endo-dig cyclization, or spiroconjugated compounds, via a 6-endo-dig cyclization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes / chemical synthesis*
  • Alkynes / chemistry
  • Catalysis
  • Cyclization
  • Cycloheptanes / chemical synthesis*
  • Cycloheptanes / chemistry
  • Iodine / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Alkynes
  • Cycloheptanes
  • Iodine
  • cycloheptanone