Rhodium carbenoid N-H insertion reactions of primary ureas: solution and solid-phase synthesis of imidazolones

Org Lett. 2003 Feb 20;5(4):511-4. doi: 10.1021/ol020244j.

Abstract

[reaction: see text] The solution and solid-phase synthesis of imidazolones is reported. The key step for the preparation of these compounds is the N-H insertion reaction of primary ureas into highly reactive rhodium carbenoid intermediates. Typically, a soluble or support-bound alpha-diazo-beta-ketoester is treated with a rhodium carboxylate catalyst in the presence of a primary urea to give the corresponding N-H insertion product. Subsequent acid-catalyzed cyclodehydration of these insertion products affords the desired imidazolone products.

Publication types

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

MeSH terms

  • Combinatorial Chemistry Techniques
  • Cyclization
  • Imidazoles / chemical synthesis*
  • Rhodium / chemistry
  • Urea / chemistry

Substances

  • Imidazoles
  • imidazolone
  • Urea
  • Rhodium