申请人:Harwood Laurence M.
公开号:US20080281075A1
公开(公告)日:2008-11-13
The present invention provides a process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S or NR
8
, where R
8
is C
1-6
alkyl, C
6-12
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.
本发明提供了一种过程,包括使用亲核试剂替换含有基团—XC(O)—的受体分子,其中X为O、S或NR8,其中R8为C1-6烷基、C6-12芳基或氢,并使受体分子环化,使得在—XC(O)—处的亲核取代反应发生而不发生对映异构化。该过程特别适用于通过从酰基氨基酸残基的活性羧基端延伸来生产肽而不发生外消旋化。