Solid-phase preparation method for buserelin

A solid-phase preparation and solid-phase synthesis technology, which is applied in the preparation methods of peptides, chemical instruments and methods, organic chemistry, etc., can solve the problems of low application value, unfavorable industrial production, complicated operation, etc., and achieves easy post-processing, The effect of less environmental pollution and simple reaction operation
CN101935339AInactive Publication Date: 2011-01-05HYBIO PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HYBIO PHARMA
Publication Date
2011-01-05
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a solid-phase preparation method for buserelin. The method comprises the following steps of: 1) preparing a Fmoc-Pro-HMPB-MBHA resin with degree of substitution of between 0.15 and 0.80mmol / g from Fmoc-Pro-OH and a HMPB-MBHA resin with degree of substitution of between 0.2 and 0.9mmol / g by a solid-phase synthesis method; 2) gradually coupling remaining protected amino acid of the Fmoc-Pro-HMPB-MBHA resin according to a peptide sequence to obtain buserelin-HMPB-MBHA resin; 3) cracking the buserelin-HMPB-MBHA resin to obtain fully-protected peptide; and 4) performing ethyl amination, deprotection and purification on the obtained fully-protected peptide to obtain buserelin. The invention aims to provide a buserelin solid-phase synthesis method which has the advantages of high yield, low cost, mild reaction conditions, small environmental pollution and contribution to realizing industrialization.
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Description

【Technical field】

[0001] The present invention relates to a method for synthesizing polypeptides, in particular to a method for solid-phase synthesis of buserelin. 【Background technique】

[0002] In the past 10 years, peptide drugs have become a hot research topic in the international pharmaceutical community, and have become the target of many manufacturers competing for development. According to a well-known international medical technology consulting company, the total output value of raw materials of peptide drugs in the world is estimated to be about 400 million US dollars. According to statistics, there are about 35 kinds of polypeptide drugs in the international market, among which the best-selling products include: buserelin, leuprolide, gorelin, luteinizing hormone antagonists and Roche's new polypeptide drug Fuzeon, etc. There are also several new active peptide drugs against SARS virus and HIV virus that will soon be approved by the US FDA. Not only American com...

Claims

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