KINETICALLY CONTROLLED PROCESS FOR ENZYMATIC PRODUCTION OF PEPTIDES

摘要

The invention pertains to a kinetically controlled process for enzymatic production of fully protected peptides formula (III): X-NH-A<1>-CO-NH-A<2>-CO-Y, wherein fully protected amino acid esters of formula (I): X-NH-A<1>-CO-Y' as acyl donor, in which X and Y' are protective groups and A<1> is an amino acid or peptide radical, are reacted with Y-protected amino acids or peptides of formula (II): NH2-A<2>-CO-Y (as nucleophiles), in which Y' is a different protective group and A<2> is an amino acid or peptide radical, in the presence of a biocatalyst (e.g. protease, preferably chymotrypsin or trypsin or (choline)-esterase), characterized in that Y' is choline or one of its salts and that the biocatalyst is an enzyme that catalyzes the cleaving to the choline-ester bond and the transfer of the acyl radical X-NH-A<1>-CO to the compound of formula (II). The choline estes lend solubility properties and efficient acyl-donor properties for the biocatalytic linkage of peptide bonds.