One-pot high-throughput synthesis of beta-turn cyclic peptidomimetics via "volatilizable" supports

J Org Chem. 2009 Mar 6;74(5):2183-5. doi: 10.1021/jo802583t.

Abstract

A promising method for the high-throughput synthesis of linear C-hydroxyalkylamido peptidomimetics and beta-turn cyclic peptidomimetics via "volatilizable" aminoalkyl functionalized silica gels is presented. Boc amino acids and carboxylic acids were coupled on functionalized aminoalkyl silica gels using a standard DIC/HOBt coupling protocol. After peptide synthesis, the resin bound peptide was cleaved using a two-step process to obtain the linear C-hydroxyalkylamido peptidomimetics. Beta-turn cyclic peptidomimetics were generated by intramolecular S(N)Ar cyclization in an aqueous solution. Both the linear and the cyclic peptidomimetics were obtained with good to excellent yields and purities through a "one-pot" reaction.

Publication types

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

MeSH terms

  • Molecular Conformation
  • Molecular Mimicry*
  • Peptides, Cyclic / chemical synthesis*
  • Peptides, Cyclic / chemistry
  • Stereoisomerism

Substances

  • Peptides, Cyclic