Study of the Mechanism of 7-exo-trig Cyclizations of Aryl, Vinyl, and Alkyl Radicals on Oxime Ethers

Carlos A. Bejarano, John E. Díaz, Jairo Camacho, Gustavo G. Flores-Bernal, Luis D. Miranda, Sol M. Mejía, Alix E. Loaiza

Research output: Contribution to journalArticlepeer-review

Abstract

In this work, we conducted a study of 7-exo-trig cyclizations mechanism involving aryl, vinyl, and alkyl radicals on oxime ethers. Initially, the reaction of brominated oxime ether 9 a with (TMS)3SiH and AIBN gave rise to aryl radicals that underwent a 7-exo-trig cyclization on the oxime ether, yielding dibenzoxepine 10 a, and the ipso reaction and reduction products were obtained as well. Approximate rate constants at 80 °C for the 7-exo-trig (1.0×108 s−1) and the ipso cyclization (4.3×107 s−1) were determined by competition experiments. DFT calculations showed good agreement with the experimental results. The reduction rate constant of the N-alkoxyaminyl radical with (TMS)3SiH was calculated to be 4.1×10−1 M−1 s−1; while the rate constants for the 7-exo-trig cyclizations of vinyl and alkyl radicals on the oxime ether were estimated in the ranges of 106 s−1–108 s−1 and 103 s−1–108 s−1, respectively. The 7-exo-trig cyclization reactions involving aryl, vinyl, and alkyl radicals with oxime ethers were found to be an exothermic and irreversible process, with the oximic carbon showing a preference for nucleophilic alkyl radicals. This kinetic study contributes to the deeper understanding of radical-mediated cyclizations, enabling the efficient design of complex synthetic routes.

Original languageEnglish
Article numbere202301148
Pages (from-to)1
Number of pages11
JournalEuropean Journal of Organic Chemistry
Volume27
Issue number7
Early online date15 Dec 2023
DOIs
StatePublished - 19 Feb 2024

Keywords

  • 7-exo-trig radical cyclizations
  • Competition experiments
  • DFT
  • Oxime ether
  • Rate constants

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