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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

Active Publication Date: 2006-11-08
SHANGHAI SOHO YIMING PHARMA
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Problems solved by technology

[0008] Chinese patent application number 02145292.X discloses a preparation method of Effibate, using Fmoc-Rink AmideAM resin as the starting material, and the fifth protected amino acid is S-triphenylmercaptopropionyl-N, N-di tert-butoxycarbonyl-homoarginine, the source of raw materials is difficult, it is not easy to prepare, and it is difficult to popularize and apply
There are defects in the use of highly toxic and corrosive reagents

Method used

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  • Process for preparing solid phase polypeptide synthetic eptifibatide
  • Process for preparing solid phase polypeptide synthetic eptifibatide
  • Process for preparing solid phase polypeptide synthetic eptifibatide

Examples

Experimental program
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Embodiment 1

[0122] Peptide chain preparation:

[0123] Weigh 72 grams of Rink Amide MBHA resin (150 mesh, 0.86mmol / g, 61.9mmol), put it into a dedicated reactor, turn on the main power supply of the synthesizer, turn on the workstation, call the pre-written peptide receiving program, soak it with 800mlDMF, Make the resin fully swell and blow dry with nitrogen. Add 800 ml of 20% hexahydropyridine in DMF and shake at 25°C for 35 minutes. Hexahydropyridine was blown and filtered with nitrogen, washed with DMF and DMF three times, and dried with nitrogen.

[0124] Preparation of Fmoc-Cys(Trt)-resin:

[0125] Add Fmoc-Cys(Trt)-OH (MW: 585.7, 2-6 times the moles of the resin) 108.9g, TBTU (MW: 321, 2-6 times the moles of the resin) 59.7g, HOBT (MW: 135.1, 2-6 times the number of moles of resin) 25.1g, NMM 41.4ml (MW=101.2), 400ml DMF, the mixture was shaken at 25°C for 1 hour. Blow dry with nitrogen, wash with DMF three times, and blow dry with nitrogen.

[0126] Add 500 ml of 20% hexahydrop...

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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.

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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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/64C07K1/04
Inventor 周达明
Owner SHANGHAI SOHO YIMING PHARMA
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