Combinatorial synthesis of libraries of indole derivatives

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2169-71. doi: 10.1016/s0960-894x(01)00393-6.

Abstract

The synthesis of two indole derivative libraries is described. 2-Acyl-3-amino-indoles 4 can easily be accessed by treatment of the intermediates 3 with bases in a one-pot reaction sequence whereas the reaction of the isolated intermediates 5 (R(3)=aromatic-, heteroaromatic, or cycloalkyl) with acid chlorides yielded the novel indole derivatives 6. The products were purified by reversed phase column chromatography and obtained in multi-milligram quantities in acceptable yields.

MeSH terms

  • Chromatography, High Pressure Liquid
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Molecular Conformation

Substances

  • Indoles