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A method for synthesizing drug polypeptide nafarelin by microwave solid-phase synthesis

A solid-phase synthesis method, the technology of nafarelin, applied in the field of solid-phase synthesis of polypeptides, can solve the problems of inconvenient yield and low reaction efficiency, and achieve the effect of convenient source, stable process and favorable industrial production

Active Publication Date: 2018-08-31
苏州强耀生物科技有限公司
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Problems solved by technology

[0003] In view of the above-mentioned technical defects, the technical problem solved by this patent is: to solve the inconvenient production process of nafarelin and the low yield and low reaction efficiency of the common solid-phase reaction method and liquid-phase reaction method

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  • A method for synthesizing drug polypeptide nafarelin by microwave solid-phase synthesis
  • A method for synthesizing drug polypeptide nafarelin by microwave solid-phase synthesis

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Embodiment Construction

[0026] 1. Preparation of Fmoc-Gly-LinkerAM Resin

[0027] Select Fmoc-Linker-AM-Resin or Fmoc-Linker-MBHA-Resin and pour it into the peptide bottle, add DCM about 2.5 times the volume of the resin, soak for 10 minutes (at room temperature), then use a vacuum pump to dry it, add the decapping reagent and put it in constant temperature oscillation React in the container for 5 minutes, dry it with a vacuum pump, re-add the capping agent and react with microwave for 3 minutes (30°C-40°C), dry it with a vacuum pump, wash with industrial grade DMF for 3 times, wash with anhydrous methanol for 3 times, and re-evaporate After washing with DCM for 3 times, add Fmoc-Gly-OH, HOBt, analytical grade DMF, and DIC to react with microwave for 5 minutes (30°C-50°C), dry it with a vacuum pump, and wash 3 times with industrial grade DMF. Wash with water and methanol for 3 times, wash with redistilled DCM for 3 times, and drain to obtain Fmoc-Gly-Linker AMResin;

[0028] The weight ratio of deca...

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Abstract

The invention relates to a method for synthesizing drug polypeptide nafarelin with a microwave solid-phase synthesis method. According to the solid-phase synthesis method, a raw material is sequentially connected with Fmoc (fluorenylmethoxy carbony) protected amino acids through a microwave reaction instrument, protective decapeptide resin is obtained, meanwhile, Fmos protecting groups are removed sequentially, one of DIC / HOBt, DIC / HOAt, BOP / HOBt, BOP / HOAt, HBTU / HOBt, HBTU / HOAt, HATU / HOBt, HATU / HOAt and HCTU / HOBt is taken as a condensing agent for a peptide synthesis reaction, side chain protecting group removing and peptide cutting are performed synchronously after the protective decapeptide resin is obtained, a crude product of nafarelin is obtained, the crude product is separated and purified by a C18 chromatographic column, the nafarelin is obtained and then subjected to freeze drying, and accordingly, a nafarelin acetate or trifluoroacetate product is obtained.

Description

technical field [0001] The invention relates to a solid-phase synthesis method of polypeptides, in particular to a method for synthesizing nafarelin. Background technique [0002] Nafarelin, also known as nafarelin acetate, is mainly used as an analogue of gonadotropin-releasing hormone (GnRH). For the treatment of endometriosis, it can eliminate pain and reduce endometrial damage. In the current conventional nafarelin production process, it often takes 1 hour to 2 hours to fully couple an amino acid to the resin. It usually takes 20 minutes to 40 minutes to remove the fmoc protecting group. From the above time data When we came out last year, it took too long to make it by conventional methods, which caused the price of the medicine to remain high. Contents of the invention [0003] In view of the above-mentioned technical defects, the technical problem to be solved by this patent is: to solve the inconvenient production process of nafarelin and the low yield and low re...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/23C07K1/06C07K1/04
CPCY02P20/55
Inventor 王锡平
Owner 苏州强耀生物科技有限公司
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