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 the 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.