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High-purity bivalirudin and industrial preparation method thereof

A technology of bivalirudin and its synthesis method, which is applied in the field of high-purity pharmaceutical peptides and its industrial preparation, can solve the problems of environmental pollution, high cost of recycling, not a washing solvent, etc., so as to reduce production costs and waste liquid discharge , the effect of low impurity content

Active Publication Date: 2014-08-06
SHENZHEN SALUBRIS PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The boiling point of DMF is as high as 152.8°C, and the cost of recycling in industrial production is relatively high. If it is discharged directly, it will cause environmental pollution; the washing effect of methanol is not good, and it cannot be used alone as a detergent. Moreover, methanol is highly toxic and easy to cause harm to people. Environmental pollution; the boiling point of dichloromethane is too low (39.8°C), and it is easy to lose due to volatilization when used alone or mixed with DMF, which is not conducive to industrial production, so it is not an ideal washing solvent
Although in actual production, the washing effect can also be improved by increasing the number of washings, but washing the resin many times will inevitably consume a large amount of organic solvents

Method used

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  • High-purity bivalirudin and industrial preparation method thereof
  • High-purity bivalirudin and industrial preparation method thereof
  • High-purity bivalirudin and industrial preparation method thereof

Examples

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Effect test

Embodiment 1

[0042] Adopt technical scheme described in the present invention to prepare bivalirudin

[0043] 1. Weigh 1 kg of Leu-Wang Resin (SD=0.60 mmol / g) resin into a silanized glass reactor, add 6 L of DMF to completely immerse the resin in it, stir for 30 min, and filter the DMF with suction. Dissolve Fmoc-Tyr-OH (0.55 kg, 1.2 mol) and HOBt (0.173 kg, 1.3 mol) in 3.3 L DMF at room temperature, add to the above resin and stir well, then add DIC (0.2 L, 1.3 mol) , stirred for 3~4 h. After detection by Kaiser reagent, the resin was colorless and the reaction solution was taken away.

[0044] 2. Add 4 L of ethyl acetate and stir for 5 minutes, then remove the washing solution.

[0045] 3. Add 5 L of 20% piperidine DMF solution by volume to the resin, stir and react for 3-10 min, and filter off the reaction solution with suction.

[0046] 4. Add 4 L of ethyl acetate and stir for 5 minutes, remove the washing solution, and repeat washing once.

[0047] 5. Add 5 L of 20% piperidine DMF...

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Abstract

The invention provides high-purity bivalirudin and an industrial preparation method thereof. The preparation method employs solid phase peptide synthesis technology and uses the solvent--ethyl acetate which is convenient to use and recover and has a low price as a washing agent, so reaction yield and product quality are improved, production cost is effectively reduced, and discharge of waste is reduced.

Description

technical field [0001] The invention belongs to a high-purity medicinal polypeptide and its industrial preparation method. In particular, the invention relates to a high-purity bivalirudin and its industrial preparation method. Background technique [0002] Bivalirudin, also known as bivalirudin, molecular formula C 98 h 138 N 24 o 33 , CAS No. 128270-60-0, is a synthetic hirudin derivative, which has the activity of inhibiting thrombin, and is often used as an anticoagulant in clinical percutaneous coronary angioplasty (PCI). Bivalirudin was first developed by Biogen, and later developed and marketed by the Medicines of the United States under the trade name Angiomax. At present, only Shenzhen Xinlitai Pharmaceutical Co., Ltd. has listed bivalirudine preparation products in China, and the trade name is taiganin. [0003] Bivalirudin consists of 20 amino acids whose amino acid sequence is: D-Phe-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-pro-Glu -Glu-Tyr-L...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/06C07K1/04
Inventor 田茂奎陈艳
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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