Metal-Free Boron-Mediated ortho-C-H Hydroxylation of N-Benzyl-3,4,5-tribromopyrazoles

Org Lett. 2022 May 20;24(19):3570-3575. doi: 10.1021/acs.orglett.2c01347. Epub 2022 May 5.

Abstract

A novel route has been reported for C-H hydroxylation of benzyl compounds directed by a 3,4,5-tribromopyrazole auxiliary via boronation/oxidation using BBr3 and NaBO3·4H2O. The strategy exhibits outstanding site selectivity and affords the corresponding phenols in moderate to excellent yields under metal-free conditions. Besides, this protocol can be achieved in one pot, which is highly promising as a practical method for use in a multistep organic synthetic process.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Boron*
  • Hydroxylation
  • Metals*
  • Oxidation-Reduction
  • Phenols

Substances

  • Metals
  • Phenols
  • Boron