Tetrahedron

Peptides containing the novel methylphosphinamide transition-state isostere

…, GA van der Marel, JH van Boom, RMJ Liskamp

Index: Moree, Wilna J.; Marel, Gijs A. van der; Boom, Jacques H. van; Liskamp, Rob M. J. Tetrahedron, 1993 , vol. 49, # 47 p. 11055 - 11064

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Citation Number: 9

Abstract

A convenient route towards the synthesis of peptides containing the methylphosphinamide moiety as a novel transition-state isostere of the amide bond hydrolysis is described. The key step being the coupling of a methylphosphinic chloride with an amino acid or peptide protected at the C-terminus. A proper choice of the amino protecting group appeared to be essential.