Fresenius Kabi Ipsum S.r.l.

Ivan Guryanov

Walter Cabri

Antonio Ricci

Andrea Orlandin

Jacopo Zanon

Fernando Formaggio

Dario Visentini

Barbara Biondi

Giuseppina Maria Incisivo

Alice Pozzebon

Angelo Viola

Andrea Borgogno

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.

Process for the manufacture of degarelix and its intermediates

The present invention provides a process for the manufacture of GLP-1 analogues with high yield and purity by fragment condensation on the solid phase. In particular, it describes a convergent synthesis by condensation of a C-terminal pseudoproline fragment A with a fragment B bound to a solid support, followed by deprotection and cleavage from the support and final purification to yield the desired peptide. The invention further provides intermediates useful in the manufacturing process.

Process for the manufacture of GLP-1 analogues

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Villadose, Italy

Ivan Guryanov