Peptide synthesis procedure in solid phase

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Synthesis of peptides

Reexamination Certificate

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C530S338000, C530S337000

Reexamination Certificate

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06897289

ABSTRACT:
A procedure for the solid phase peptide synthesis (SPPS), following a linear or convergent strategy, wherein the peptides contain the sequence of general formula (I), wherein n, Y, X and A1to Anhave the meanings indicated in the specification. Said procedure comprises: the use of amino acids with the Nα group protected, protecting the side chains of those amino acids that have their side chain alkylated or acylated in the final product with labile protecting groups, protecting the side chains of at least one of the amino acids that has its chain free in the final product with hyperlabile products and using a polymeric support which provides labile peptide-resin bonds.Said procedure is valid for the synthesis of gosereline and buserelinein-line-formulae description="In-line Formulae" end="lead"?Y—A1—A2—A3— . . . A(n-1)—An—X.in-line-formulae description="In-line Formulae" end="tail"?

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Lloyd-Williams et al., “Convergent Solid-Phase Peptide Synthesis”, 1993, in Tetrahedron, 49(48), pp. 11065-11133.*
Alberico et al., “Convergent Solid-Phase Peptide Synthesis”, 1997, in Methods in Enzymology, vol. 289, Chapt. 15, pp313-336, ed. Fields, Academic Press, New York.*
A. Friedrich et al., “Experiences During the Development of the Buserelin Acetate Synthesis,” Peptides 1992, pp. 47-49 (C.H. Schneider and A.N. Eberle, Eds.), 1993 ESCOM Science publishers B.V.

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