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Preparation method of polypeptide

A peptide resin and resin technology, applied in the field of polypeptide preparation, can solve problems such as no large-scale synthesis method, no known synthesis method, etc.

Inactive Publication Date: 2016-04-20
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] At present, there is no report on the synthesis method, let alone a large-scale synthesis method

Method used

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[0037] The invention discloses a preparation method of a polypeptide, and those skilled in the art can learn from the content of this article and appropriately improve the process parameters to realize it. In particular, it should be pointed out that all similar replacements and modifications are obvious to those skilled in the art, and they are all considered to be included in the present invention. The method and application of the present invention have been described through preferred embodiments, and the relevant personnel can obviously make changes or appropriate changes and combinations to the method and application described herein without departing from the content, spirit and scope of the present invention to realize and Apply the technology of the present invention.

[0038] The amino acids and reagents used in the preparation method of the polypeptide provided by the present invention can be purchased from the market.

[0039] Abbreviation and English meaning

[...

Embodiment 1

[0053] Embodiment 1: the degree of substitution is the synthesis of Fmoc-D-Arg (pbf)-amino resin of 0.5mmol / g

[0054]Weigh 400 g of RinkAmidoresin with a substitution degree of 1.0 mmol / g, add it to a solid-phase reaction column, wash it twice with DMF, and swell the resin with DMF for 30 minutes. The Fmoc protection was deprotected with DBLK (20% piperidine / DMF), followed by 4 washes with DMF and 2 washes with DCM. Weigh 162.2g of Fmoc-D-Arg(pbf)-OH (250mmol) and 40.5g of HOBt (300mmol) and dissolve it in a mixed solution of DCM and DMF with a volume ratio of 1:1, add 46.9ml of DIC (300mmol) under an ice-water bath for activation for 3 minutes, and then add In a solid-phase reaction column, react at room temperature for 2 hours. Wash 3 times with DMF, add 1395.1ml of blocking solution (pyridine / acetic anhydride = 1:1, 8mol:8mol) to block for 8 hours (if the resin is not fully diffused, add DCM as a solvent). Wash 4 times with DMF, 4 times with DCM, shrink and dry with meth...

Embodiment 2

[0057] Embodiment 2: the degree of substitution is the synthesis of Fmoc-D-Arg (pbf)-amino resin of 0.2mmol / g

[0058] Weigh 400 g of RinkAmidoresin with a substitution degree of 1.0 mmol / g, add it to a solid-phase reaction column, wash it twice with DMF, and swell the resin with DMF for 30 minutes. The Fmoc protection was deprotected with DBLK (20% piperidine / DMF), followed by 4 washes with DMF and 2 washes with DCM. Weigh 64.9g of Fmoc-D-Arg(pbf)-OH (100mmol) and 16.2g of HOBt (120mmol) and dissolve it in a mixed solution of DCM and DMF with a volume ratio of 1:1, add 18.8ml of DIC (120mmol) under ice-water bath for activation for 3min and then add In a solid-phase reaction column, react at room temperature for 2 hours. Wash 3 times with DMF, add 1395.1ml of blocking solution (pyridine / acetic anhydride = 1:1, 8mol:8mol) to block for 8 hours (if the resin is not fully diffused, add DCM as a solvent). Wash 4 times with DMF, 4 times with DCM, shrink and dry with methanol to o...

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Abstract

The invention relates to the field of polypeptide, and especially relates to a preparation method of polypeptide. The preparation method comprises the following steps: coupling Arg with resin to prepare Arg-resin; individually coupling Arg-resin with Ala, Arg, Arg, Arg, Ala, and Cys (X) in sequence, carrying out amino acetylation on the nitrogen terminal to obtain a first peptide resin; removing the side chain protective group X in Cys (X) of the first peptide resin, then coupling the first peptide resin with Y-Cys to obtain a second peptide resin, and cracking the second peptide resin to obtain the polypeptide. The preparation method is carried out in pure solid state, the operation is simple and convenient, and the pseudo-dilution effect avoid the disulfide bond mispairing reactions between polypeptide chains in liquid phase reactions ( no reactions happens between peptide chains). The yield and purity of polypeptide Velcalcetide are both improved, and the side reactions are reduced.

Description

technical field [0001] The invention relates to the field of polypeptides, in particular to a preparation method of polypeptides. Background technique [0002] Velcalcetide, also known as AMG416, has the amino acid sequence shown in SEQ ID No.1 and the structure shown in Formula I. [0003] [0004] Velcalcetide for secondary hyperparathyroidism in patients with chronic kidney disease receiving dialysis. The drug is currently undergoing Phase III studies, and research data are expected to be released in the second half of 2014. [0005] Amgen already has a drug on the market for the same indication, called Sensipar. Sales of the drug rose 14.6 percent to $1.09 billion last year. [0006] Velcalcetide can be given intravenously while undergoing hemodialysis, which is a boon for chronic kidney disease patients who need to use large amounts of the drug every day. Therefore, velcalcetide is likely to surpass its predecessor Sensipar. Analysts expect peak annual sales of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/06C07K1/04
CPCY02P20/55
Inventor 宓鹏程刘建马亚平袁建成
Owner HYBIO PHARMA
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