Research Corporation Technologies, Inc.

Ayman Ahmed El-Faham

Louis A Carpino

Synthesis and use of amino acid fluorides as peptide coupling reagents

The present invention is directed to a process for forming a peptide bond between a first amino acid having a free amino group and a protected carboxy group and a second amino acid or between a peptide having a free amino group and a blocking carboxy group with a second amino acid which comprises (a) reacting the second amino acid of the formula: ##STR1## with a fluoroformamidinium salt of the formula: ##STR2## and (b) reacting the product of (a) with the first amino acid or peptide.

Synthesis and use of amino acid fluorides as peptide coupling reagent

The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting group

The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting group AA is an amino acid residue and X is H or a protecting group useful, and the first amino and peptide have a free amino group and a blocked carboxy end.

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Amherst, MA, United States of America

Ayman Ahmed El-Faham