ASYMMETRIC SYNTHESIS OF PEPTIDES

摘要

The present invention provides a process comprising substitution of an acceptor molecule comprising a group -XC(O)- wherein X is O, S or NR<SUP>8</SUP>, where R<SUP>8</SUP> is C<SUB>1-6</SUB> alkyl, C<SUB>6-12</SUB> aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at -XC (O)- occurs without racemisation. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.