Preparation method of solid phase synthesis cetrorelix

Abstract

A method for realizing the solid phase synthesis of cetrorelix comprises the following steps that: Fmoc-Linker-MBHA-Resin is used as a starting raw material and is connected in turn with amino acid with Fmoc-protecting groups according to a solid phase synthesis method, so as to obtain protective decapeptide resin; meanwhile, the Fmoc-protecting groups are divested in turn; one sort of HBTU / HOBT or DIC / HOBT is used as condensing agent to carry out synthesized peptide, thereby obtaining protective decapeptide resin; acetylation reaction is carried out, and then protecting group side chain divesting and peptide cutting are carried out synchronously to obtain cetrorelix acetate which is separated and purified through C18 or C8 chromatographic column; finally, cetrorelix acetate acetate or trifluoroacetate is obtained after freeze drying.

Description

Technical field:

[0001] The invention relates to a preparation method of cetrorelix acetate (including acetate, trifluoroacetate and free peptide), especially a preparation method of solid-phase polypeptide synthesis of cetrorelix. Background technique:

[0002] Chinese name: Cetrorelix acetate

[0003] English name: Cetrorelix Acetate

[0004] Structural formula:

[0005] AC-3-(2-naphthyl)

[0006] -D-Ala-4-Chloro-D-Phe-3(3-Pyriclyl-D-Ala-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH2

[0007] Molecular formula and molecular weight: C70H92N17O14CL 1430.1

[0008] Cetrorelix Acetate is a gonadotropin-releasing hormone used to stimulate regulated ovaries prior to infertility treatment. The main treatment is gonadotropin-releasing hormone receptor blockade.

[0009] The effect of LHRH antagonist Cetrorelix on the growth cycle and cycle-related proteins of endometrial cancer cells, and to explore its mechanism of inhibiting the growth of endometrial cancer cells

[0010] Solvay, a ...