Solid phase preparation method of carbetocin

A technology of carbetocin and solid-phase synthesis, which is applied in the field of solid-phase synthesis of polypeptides, and achieves the effects of simple reaction operation, high yield, and easy post-processing
CN101555272BActive Publication Date: 2012-05-09HYBIO PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HYBIO PHARMA
Publication Date
2012-05-09

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Abstract

The invention discloses a solid phase synthesis method of carbetocin. The technical proposal comprises the following steps of: obtaining Fmoc-Gly-amino resin by reaction of Fmoc-Gly-OH and amino resinwith the substitutability being 0.2 mmol / g-0.9 mmol / g; sequentially connecting amino acids with Fmoc protecting groups by the solid phase synthesis method to obtain carbetocin precursor peptide I-amino resin; stripping off cysteine side chain protecting groups to obtain carbetocin precursor peptide II-amino resin; adding organic alkali and lithium chloride in solvent for cyclization to obtain carbetocin-amino resin; cracking to obtain carbetocin crude peptide; and purifying and freeze-drying to obtain the carbetocin. The method adopts the amino resin to synthesize carbetocin by the solid phase cyclization technology. The process is characterized by simple operation, easy post-treatment, high yield, low cost, and the like, and has considerable economical and practical value and broad application prospect.
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Description

technical field

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

[0002] Carbetocin is a synthetic long-acting nonapeptide analogue of oxytocin with agonist properties. A single dose intravenously may be administered immediately after cesarean section under epidural or spinal anesthesia to prevent uterine hypotonia and postpartum hemorrhage. The clinical trial jointly completed by Peking Union Medical College Hospital, Peking University First Affiliated Hospital and Beijing Obstetrics and Gynecology Hospital showed that compared with the traditional continuous infusion of oxytocin to control bleeding after elective cesarean section, the drug has less bleeding after 24 hours. There was no significant difference in blood loss, and there was no significant difference in total intraoperative and postoperative blood loss; there was no significant difference between the...

Claims

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