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February 8, 2026Organic Letters0 citations

Rhodium-Catalyzed Formal C–H and X–H Insertion Reaction Involving an Exocyclic Vinylic Cation Intermediate

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KHKemiao HongJHJie HeJLJingxian Li

Key Points

  • The study aims to explore selective transformations involving exocyclic vinylic carbocations through Rh-catalysis.
  • Utilized Rh-catalyzed formal C-H and X-H insertion reactions
  • Generated exocyclic vinylic cations in situ
  • Tested a range of nucleophiles for reaction yield
  • Achieved reactions under mild conditions with a broad substrate scope
  • Successfully synthesized tetrasubstituted alkenes with a cyclobutanone motif
  • Produced 3-methylenecyclobutanone derivatives, which are challenging to obtain by other methods
  • Demonstrated the utility of the method for postfunctionalization transformations

Abstract

The carbocation is one of the highly reactive intermediates in synthetic chemistry; however, catalytic selective transformations involving vinylic cation species remain elusive in comparison to sp2-hybrid ones. Herein, we report a Rh-catalyzed formal C-H and X-H insertion reaction of in situ-generated exocyclic vinylic cations with a variety of nucleophiles, affording tetrasubstituted alkenes incorporating a cyclobutanone motif with a broad substrate scope under mild conditions. The utility of this method has been demonstrated for the synthesis of 3-methylenecyclobutanone derivatives, which are difficult to access using other methods, serving as versatile building blocks for a range of postfunctionalization conversions.

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Cite This Study

Hong et al. (2026) studied this question.

synapsesocial.com/papers/698827b40fc35cd7a8846ad3https://doi.org/10.1021/acs.orglett.5c05314
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