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Preparation method for synthesizing proteidin with solid phase polypeptide

A solid-phase peptide synthesis, proteolysin technology, applied in the preparation methods of peptides, chemical instruments and methods, peptides and other directions

Active Publication Date: 2012-02-01
SHANGHAI SOHO YIMING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there is no report on the industrial production technology of polypeptide products containing two pairs of disulfide bonds. Therefore, this technology has great practical significance

Method used

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  • Preparation method for synthesizing proteidin with solid phase polypeptide

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Embodiment 1

[0117] (1) Preparation of Fmoc-Arg(Pbf)-resin

[0118] Weigh 200 grams of Rink Amide MBHA resin (200 mesh, 0.50 mmol / g, 100 mmol), soak it with 2000 ml DMF to fully swell the resin, and drain it. Add 1600 ml of 23% hexahydropyridine in DMF and react at 22-24°C for 30 minutes. Drain, wash with DMF, anhydrous methanol, and DMF three times respectively, and drain.

[0119] Add Fmoc-Arg(Pbf)-OH (MW: 648.8, 200mmol) 130g, HBTU (MW: 321, 200mmol) 64.2g, HOBT (MW: 153.1, 200mmol) 30.6g, NMM 50ml (MW= 101.2), react the mixture at 22-24°C for 70 minutes. Drain, wash with DMF, anhydrous methanol, and DMF three times each, and drain.

[0120] (2) Preparation of Fmoc-Gly-Arg(Pbf)-resin

[0121] Add 1600 ml of 23% hexahydropyridine in DMF and react at 22-24°C for 30 minutes. Drain, wash with DMF, anhydrous methanol, and DMF three times respectively, and drain.

[0122] Add 59.5g of Fmoc-Gly-OH (MW: 297.3, 200mmol) dissolved in 1600ml of DMF, 64.2g of HBTU (MW: 321, 200mmol), 30.6g of...

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Abstract

The invention discloses a preparation method for synthesizing proteidin with a solid phase peptide. The technical scheme of the invention comprises the following steps of: connecting amino acids with Fmoc-protection groups in sequence by taking Rink Amide MBHA resin as an initial raw material and taking HBTU / HOBt as a concentration agent according to a solid phase synthesis method to obtain protected heptadeca-peptide resin, wherein Boc-Arg-OH.HCl is taken as a last amino acid; adding a peptide cutting reagent for cutting peptides; adding diethyl ether for precipitating to obtain a reduced crude product; protecting the -SH groups of 5-bit and 14-bit Cys with Trt; oxidizing with hydrogen peroxide at the pH 8.5-10.0; protecting the -SH groups of 7-bit and 12-bit Cys with Acm; oxidizing with iodine in a methanol solution to obtain a dual disulfide bond Cys5-14Cys7-12 crude product; and separating by adopting a C8 high-efficiency liquid phase column for purifying to obtain a target product, wherein the purity of the target product is 99.21 percent, and the total yield is 23.68 percent. The method has the advantages of low production cost, simple process, low environmental pollution, high yield and convenience for industrial implementation.

Description

technical field [0001] The invention relates to a preparation method of proteolysin, in particular to a solid-phase polypeptide synthesis preparation method of proteolysin. Background technique [0002] Chinese name: proteolysin [0003] English name: Protegrin, Iseganan [0004] Structural formula: [0005] [0006] Molecular formula: C 78 h 126 N 30 o 18 S 4 ·HCl [0007] Molecular weight: 1900.32 + 36.46 [0008] CAS number: 256475-21-5 [0009] Protein lysin exists naturally in mammals and is distributed in the front line of bacterial and fungal invasion. It has broad-spectrum antimicrobial activity and can minimize the possibility of microbial drug resistance. Intra Biotics pharmaceutical company's phase I clinical trial in the United States believes that it is a promising new drug for the treatment of cystic fibrosis (CF), and the experimental dosage form is designed as an oral antibiotic solution. The drug is currently in phase III clinical trials, and i...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/20C07K1/06C07K1/04
Inventor 周逸明崔颀蔡华成
Owner SHANGHAI SOHO YIMING PHARMA
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