| 摘要 |
<p>Dipeptides H-A-B-Y, wherein A is an α- or φ-amino acid residue, B is an α-aminocarboxylic, aminophosphonic acid or aminosulfonic acid residue, and Y is OH, H or a C-terminal protective group, are produced by reacting a substrate component: H-A-OR1 or H-A-NR2R3, wherein R?1, R2, R3¿ are alkyl, aryl or aralkyl or R?2 and R3¿ are H, with a nucleophile component selected from aminocarboxylic acids or their amides, esters, aldehydes or ketones: H-B-NR2R3, H-B-OR4 or H-B-R8, wherein B, R?2 and R3¿ are as defined above, R?4 and R8¿ are alkyl, aryl or aralkyl or R8 is H, or aminophosphonic or aminosulfonic acids, in the presence of an amidase or esterase enzyme different from serine or thiol carboxypeptidases, preferably a serine or thiolendoprotease, lipase, esterase or glycosidase in solution or dispersion, and then, if desired, cleaving a present side-chain protecting group or protective group Y. The process allows for production of LL-, LD-, DL- and DD-dipeptides without risk of racemization in a simple and economic manner.</p> |
