Copper- and palladium-catalyzed intramolecular aryl guanidinylation: an efficient method for the synthesis of 2-aminobenzimidazoles

Org Lett. 2003 Jan 23;5(2):133-6. doi: 10.1021/ol027061h.

Abstract

[reaction: see text] The formation of 2-aminobenzimidazoles via intramolecular C[bond]N formation between an aryl halide and a guanidine moiety can be achieved using either copper or palladium catalysis. Inexpensive copper salts such as CuI are generally superior to the use of palladium catalysts. Regioselective cyclizations, where R(3) = H, can be achieved in high yield under CuI/1,10-phenanthroline-catalyzed conditions, whereas palladium catalysis results in the formation of regioisomeric products.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzimidazoles / chemical synthesis*
  • Catalysis
  • Copper / chemistry
  • Cyclization
  • Guanidine / chemistry*
  • Palladium / chemistry

Substances

  • Benzimidazoles
  • Palladium
  • Copper
  • 2-aminobenzimidazole
  • Guanidine