Multicomponent type II anion relay chemistry (ARC): one-pot syntheses of 2,3-disubstituted furans and thiophenes

Org Lett. 2009 Apr 16;11(8):1861-4. doi: 10.1021/ol900434k.

Abstract

Effective, one-pot syntheses of 2,3-disubstituted furans and thiophenes, exploiting 2-tert-butyldimethylsilyl-3-formylfuran and -thiophene as the respective bifunctional linchpins, have been developed. The synthetic protocol involves multicomponent type II Anion Relay Chemistry (ARC) mediated by a solvent-controlled C(sp(2))-->O 1,4-Brook rearrangement. Simple organolithiums and alpha-disubstituted ester enolates prove effective as the initiating nucleophiles.

Publication types

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

MeSH terms

  • Anions
  • Combinatorial Chemistry Techniques
  • Furans / chemical synthesis*
  • Furans / chemistry
  • Lithium / chemistry
  • Molecular Structure
  • Organometallic Compounds / chemistry
  • Thiophenes / chemical synthesis*
  • Thiophenes / chemistry

Substances

  • Anions
  • Furans
  • Organometallic Compounds
  • Thiophenes
  • Lithium