Millennium Pharmaceuticals Limited

Polypeptide Laboratories Holding (ppl) Ab

Lonza Braine Sa

Lonza Inc.

Lonza Ag

Polypeptide Laboratories Holding Ab

Luciano Forni

Guojie Ho

Fernando Albericio Palomera

Daniel Carbajo Lopez

Geoffroy Sommen

Antoinette D Paone

Catherine De Tollenaere

Brice Bonnet

Christine Devijver

Didier Monnaie

Catherine Detollenaere

Vincent Cool

Alain Ronvaux

The invention discloses a method for the preparation of a peptide by liquid phase coupling of two fragments, an N-terminal fragment and a C-terminal fragment of the desired peptide, wherein the C-terminal fragment is protected on its C-terminal COOH by a psWang linker; the method is demonstrated with liraglutide wherein the C-terminal fragment carries the Palmitoyl-Glu-OtBu residue on the Lys.

Method for preparation of peptides with psWang linker

The present invention relates to a process for the production of bivalirudin, a 20-mer peptide of formulaH-(D)-Phe-Pro-Arg-Pro-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu-OH (SEQ ID NO: 1).

Process for the production of bivalirudin

The present invention provides, inter alia, convergent processes for preparing eptifibatide that involve coupling a 2-6 eptifibatide fragment to an activated cysteinamide residue to form a 2-7 eptifibatide fragment, attaching a mercaptopropionic acid residue to the 2-7 eptifibatide fragment through disulfide bond formation, coupling the peptide intramolecularly, and removing the protecting group, to form eptifibatide. The invention further provides products produced by the described processes, novel compounds that can be used as synthetic intermediates for the preparation of eptifibatide, and novel compounds that are structurally similar to eptifibatide.

Processes for preparing eptifibatide

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La Louvière, Belgium

Luciano Forni