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Solid-phase synthesis method for eptifibatide

A technology of solid-phase synthesis of eptifibatide, applied in peptide preparation methods, chemical instruments and methods, peptides, etc., can solve the problems of large environmental pollution and long liquid-phase synthesis cycle, etc., achieve simple operation and shorten production cycle , The effect of saving production costs

Active Publication Date: 2010-09-22
YANCHENG KAILI PHARMA
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0005] At present, the foreign manufacturer of this product is Bachem company in Switzerland. The synthesis route of Bachem company is the liquid phase synthesis method and the BOC strategy method. The liquid phase synthesis cycle is relatively long, and the BOC synthesis method causes great environmental pollution.

Method used

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  • Solid-phase synthesis method for eptifibatide

Examples

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Embodiment 1

[0033] 1. Preparation of Fmoc-Cys(trt)-Linker-AM resin

[0034] Wash the Fmoc-Linker-AM resin twice with DMF, then soak it in DCM for about 10 minutes to fully swell the resin, add 25% piperidine, react for 20 minutes, drain it, and wash it three times with DMF and DCM , add Fmoc-Cys(trt)-OH dissolved in DMF 2 The mixture of / HOBt / DIC was reacted at room temperature for 2 hours, drained, and then washed alternately with DMF and DCM three times to obtain the Fmoc-Cys(trt)-Linker-AM resin. The amount of amino acid and condensation reagent used is two times excess of the molar coefficient of resin; the following process is the same.

[0035] 2. Preparation of Fmoc-Pro-Cys(trt)-Linker-AM resin

[0036] After the above steps, add 25% piperidine to react for 20 minutes, wash with DMF and DCM alternately three times, drain, add Fmoc-Pro-OH dissolved in DMF 2 The mixture of / HOBt / DIC / DMAP was reacted at room temperature for 2 hours, drained, and then alternately washed three times ...

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Abstract

The invention discloses a solid-phase synthesis method for eptifibatide. The solid-phase synthesis method for the eptifibatide comprises the following steps of: carrying out amino acid condensation on carrier resin, drying the obtained resin, and cutting the resin with trifluoroacetic acid to obtain an eptifibatide coarse product; oxidizing the eptifibatide coarse product with hydrogen peroxide for 30 to 60 minutes; neutralizing with acetic acid, filtering the mixture, carrying out HPLC purification on the filtrate, and collecting characteristic peaks; and distilling, concentrating and freeze-drying collections to obtain an acetic acid eptifibatide refined product. The invention provides a simple and easily operated process synthesizing route, and only needs monoprotected Fmoc-Har-OH2 and Fmoc-Trp-OH2 when raw materials are selected during synthesizing so as to easily obtain the raw materials and shorten production cycle.

Description

technical field [0001] The present invention relates to the preparation method of medicine, specifically, the present invention is a kind of solid-phase synthetic method of eptifibatide. Background technique [0002] Eptifibatide is a cyclic peptide containing one mercaptopropionic acid and six amino acid residues, its formula: C 35 h 49 N 11 o 9 S 2 , its sequence is: [0003] [0004] Eptifibatide is an anticoagulant drug in the vascular and blood system drugs. It is a colorless amorphous amorphous white powder and is easily soluble in water. Its main function is to selectively block the combination of glycoprotein IIb / IIIa and adhesion proteins, and has a certain weak inhibitory effect on adhesion-related receptors. Platelet aggregation plays a role in preventing. [0005] At present, the foreign manufacturer of this product is Bachem Company in Switzerland. The synthesis route of Bachem Company is the liquid phase synthesis method and the BOC strategy method. T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/04A61P7/02
Inventor 廖志杨毅跃
Owner YANCHENG KAILI PHARMA
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