Design and Development of the First Peptide-Chelating Bisphosphane Bioconjugate from a Novel Functionalized Phosphorus(III) Hydride Synthon

Abstract

Remarkable oxidative stability is shown by the carboxylate-functionalized primary bisphosphane 1. Compound 1 can be used in conjugation reactions with biomolecules for functionalization through the COOH group without prior protection of PH₂ groups. A novel water-soluble bisphosphane was obtained by reaction of the PH₂ groups of 1 with formaldehyde under mild conditions.