Process for the manufacture of degarelix and its intermediates
AssigneeFresenius Kabi Ipsum S.R.L.
InventorsAntonio Ricci, Jacopo Zanon, Walter Cabri, Ivan Guryanov, Andrea Orlandin, Barbara Biondi, Fernando Formaggio, Dario Visentini
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Abstract
The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.
Claims13
A method for preparing degarelix of formula I,
- or a pharmaceutically acceptable salt thereof, comprising incorporating a nitro-peptide comprising one or two p-nitrophenylalanine residues into a precursor peptide, and transforming the one or two p-nitrophenylalanine residues into Aph(Hor) or Aph(Cbm) in the precursor peptide, and converting the precursor peptide into degarelix or a pharmaceutically acceptable salt thereof and, wherein the method is performed as solid phase peptide synthesis.
A method for preparing degarelix of formula I,
- or a pharmaceutically acceptable salt thereof, wherein the method comprises the use of a nitro-peptide comprising one or two p-nitrophenylalanine residues, followed by modification of the one or two p-nitrophenylalanine residues incorporated in the peptide sequence into the respective Aph derivative Aph(Hor) or Aph(Cbm), and wherein the method is performed as solid phase peptide synthesis.
Dependencies are inferred from the claim text.