A novel process for the amidation or esterification which comprises reacting a compound having a carboxy group with a compound having an amino or imino group which can be acylated or with a compound having a hydroxy group in the presence of a sulfonic acid ester of the formula: R.sub.1 --SO.sub.2 --OR.sub.2 wherein R.sub.1 is an organic group and R.sub.2 O-- is a residue of a strongly acidic N-hydroxy compound as a condensation agent, and a novel sulfonic acid ester useful as such a condensation agent and a process for the preparation thereof.
Tandem deprotection/coupling for peptide synthesis in water at room temperature
作者:Margery Cortes-Clerget、Jean-Yves Berthon、Isabelle Krolikiewicz-Renimel、Laurent Chaisemartin、Bruce H. Lipshutz
DOI:10.1039/c7gc01575e
日期:——
A tandem deprotection/coupling sequence is reported for solution-phasepeptidesynthesis in water under micellar catalysis conditions using the designer surfactant TPGS-750-M. Cbz deprotection followed by peptide coupling in the presence of COMU and 2,6-lutidine afforded polypeptides containing up to 10 amino acid residues. A broad scope characterizes this new technology. No epimerization has been