Bismuth Acetate as a Catalyst for the Sequential Protodeboronation of Di- and Triborylated Indoles

Org Lett. 2016 Apr 1;18(7):1554-7. doi: 10.1021/acs.orglett.6b00356. Epub 2016 Mar 21.

Abstract

Bismuth(III) acetate is a safe, inexpensive, and selective facilitator of sequential protodeboronations, which when used in conjunction with Ir-catalyzed borylations allows access to a diversity of borylated indoles. The versatility of combining Ir-catalyzed borylations with Bi(III)-catalyzed protodeboronation is demonstrated by selectively converting 6-fluoroindole into products with Bpin groups at the 4-, 5-, 7-, 2,7-, 4,7-, 3,5-, and 2,4,7-positions and the late-stage functionalization of sumatriptan.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Acetates / chemistry*
  • Bismuth / chemistry*
  • Boron Compounds / chemistry*
  • Catalysis
  • Indoles / chemistry*
  • Molecular Structure

Substances

  • Acetates
  • Boron Compounds
  • Indoles
  • Bismuth