Stereoselective Synthesis of Highly Functionalized Cyclohexenes via Strong-Acid-Mediated Endocyclic C-C Bond Cleavage of Monocyclopropanated Cyclopentadienes

Org Lett. 2023 Jun 23;25(24):4411-4415. doi: 10.1021/acs.orglett.3c00935. Epub 2023 May 30.

Abstract

A stereoselective, solvent- and metal-free endocyclic C-C bond cleavage of monocyclopropanated cyclopentadienes mediated by strong acids was developed, leading to highly functionalized six-membered carbocycles with high stereocontrol. The critical step for this ring-expansion is the formation of a cyclopropyl carbocation that undergoes endocyclic ring opening via an SN2'-type attack of various nucleophiles. Subsequent synthetic transformations show the versatility of the resulting cyclohexenes for the synthesis of new compounds with nonconventional substitution patterns.

MeSH terms

  • Cyclization
  • Cyclopentanes*
  • Solvents / chemistry
  • Stereoisomerism

Substances

  • Cyclopentanes
  • Solvents