Benzoylureas as removable cis amide inducers: synthesis of cyclic amides via ring closing metathesis (RCM)

Org Biomol Chem. 2011 Feb 7;9(3):656-8. doi: 10.1039/c0ob00723d. Epub 2010 Nov 18.

Abstract

Rapid and high yielding synthesis of medium ring lactams was made possible through the use of a benzoylurea auxiliary that serves to stabilize a cisoid amide conformation, facilitating cyclization. The auxiliary is released after activation under the mild conditions required to deprotect a primary amine, such as acidolysis of a Boc group in the examples given here. This methodology is a promising tool for the synthesis of medium ring lactams, macrocyclic natural products and peptides.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis*
  • Benzene / chemistry*
  • Cyclization
  • Molecular Structure
  • Urea / chemistry*

Substances

  • Amides
  • Urea
  • Benzene