Process for preparing solid phase polypeptide synthetic eptifibatide

A technology of solid-phase peptide synthesis and Effibate, which is applied in peptide preparation methods, chemical instruments and methods, and peptides, and can solve problems such as difficult source of raw materials, use, and difficulty in preparation
CN1858060AActive Publication Date: 2006-11-08SHANGHAI SOHO YIMING PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI SOHO YIMING PHARMA
Publication Date
2006-11-08

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Abstract

The preparation process of solid phase polypeptide synthesized eptifibatide includes the following steps: (1) connecting amino acids one by one with Rink Amide resin, Rink Amide MBHA resin or Rink Amide AM resin as initial material, and Fmoc protected amino aids as monomer, with the last peptide chain being S-benzyl mercapto propionic acid Map(SBzl); (2) adding peptide cutting agent (TFA / HBr / HAc / TIS / EDT) to cut peptide; (3) precipitating and collecting coarse reductant eptifibatide product in ether solvent; (4) dissolving coarse reductant eptifibatide product in water, regulating pH value with ammonia water to 7.5-10.0, introducing air for oxidation, and collecting coarse eptifibatide product; and (5) separating and purifying the coarse product in C18 column to obtain the target product. The present invention has high yield, and is suitable for industrial production.
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Description

technical field

[0001] The invention relates to a preparation method of efibate, in particular to a preparation method of solid-phase polypeptide synthesis efibate. Background technique

[0002] Eptifibatide, the English name is Epifibatide, and its structural formula is:

[0003]

[0004] Molecular formula is C 35 h 49 N 11 o 9 S 2

[0005] Efibate is clinically a specific GP IIb / IIIa receptor antagonist that can be injected intravenously. By preventing fibrin from binding to GP IIb / IIIa receptors, thereby inhibiting platelet aggregation and preventing thrombosis, this product is clinically used as an adjuvant drug for heparin or aspirin.

[0006] Effibate is a synthetic cyclic heptapeptide, an antagonist of platelet glycoprotein GP IIb / IIIa receptors, which can block the platelet aggregation reaction caused by various activators, and is the strongest specific platelet aggregation inhibitor known It is mainly used to prevent myocardial oxygen supply artery occlus...

Claims

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