| 摘要 |
The present invention relates to processes and intermediates useful for the manufacture of cyclic undecapeptides, such as Alisporivir, a non-immunosuppressive cyclosporine A derivative. The cyclosporin is acylated on the butenyl-methyl-threonine side chain and then subjected to a ring-opening reaction (the ring opens between the sarcosine and the N-methyl-leucine residues). This linear peptide intermediate is subjected to Edman degradation (removal of the N-terminal residue) as to give the second linear decapeptide intermediate, e.g. of sequence Val-N(Me)Leu-Ala-Ala-N(Me)Leu-N(Me) Leu-N(Me)Val-N(Me)Bmt-Abu-Sar when starting from CsA. |
