Synthesis 2017; 49(04): 891-898
DOI: 10.1055/s-0035-1562619
paper
© Georg Thieme Verlag Stuttgart · New York

Synthesis of Oxindoles and Benzofuranones via Oxidation of 2-Heterocyclic BMIDAs

Ciaran P. Seath
Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde, 295 Cathedral St., Glasgow, G1 1XL, UK   Email: allan.watson.100@strath.ac.uk
,
James W. B. Fyfe
Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde, 295 Cathedral St., Glasgow, G1 1XL, UK   Email: allan.watson.100@strath.ac.uk
,
John J. Molloy
Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde, 295 Cathedral St., Glasgow, G1 1XL, UK   Email: allan.watson.100@strath.ac.uk
,
Allan J. B. Watson*
Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde, 295 Cathedral St., Glasgow, G1 1XL, UK   Email: allan.watson.100@strath.ac.uk
› Author Affiliations
Further Information

Publication History

Received: 14 June 2016

Accepted after revision: 22 July 2016

Publication Date:
12 August 2016 (online)


Abstract

The synthesis of functionalized oxindoles and benzofuranones via oxidation of 2-BMIDA indoles and benzofurans, respectively, is described. Interconversion of boron species (BMIDA→BF3K) was necessary to enable oxidation and overcome boronic acid stability issues associated with a difficult BMIDA hydrolysis. Overall, a robust process was developed that allowed access to a small library of oxindole and benzofuranone products and facilitated the step-efficient synthesis of biologically active compounds containing the oxindole pharmaco­phore.

Supporting Information