WO2026107622 - METHOD FOR SYNTHESIZING SEMAGLUTIDE
National phase entry is expected:
Publication Number
WO/2026/107622
Publication Date
28.05.2026
International Application No.
PCT/CN2024/132863
International Filing Date
19.11.2024
Title **
[English]
METHOD FOR SYNTHESIZING SEMAGLUTIDE
[French]
PROCÉDÉ DE SYNTHÈSE DE SÉMAGLUTIDE
[Chinese]
一种司美格鲁肽的合成方法
Applicants **
SHENZHEN JYMED TECHNOLOGY CO., LTD
Inventors
YAO, Zhiyong
LI, Xinyu
FU, Yuqing
MA, Hongji
ZHANG, Lixiang
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1703 | |
| EPO | Filing, Examination, Granting | 12624 | |
| Japan | Filing, Examination, Granting | 2243 | |
| South Korea | Filing, Examination, Granting | 2145 | |
| USA | Filing, Examination, Granting | 4740 |
Total:
23,455
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Abstract[English]
Provided is a method for synthesizing semaglutide. The method mainly comprises: coupling a resin with a protected amino acid and a polypeptide fragment by means of a solid phase synthesis method to obtain a semaglutide peptide resin, and performing cleavage and purification on the semaglutide peptide resin to obtain the semaglutide, wherein the fragment comprises Gly29-Arg30, R1-Lys[AEEA-AEEA-γGlu(OR2)-C18-R3]-OH, Glu15-Gly16, Thr5-Phe6, and His1-Aib2-Glu3-Gly4. The method effectively avoids the occurrence of DKP side reactions, increases the resin weight gain rate to 98% or more, ameliorates the problem of difficult coupling caused by β-sheets, and effectively avoids the generation of impurities. In the crude peptide, the content of [D-His1] semaglutide does not exceed 0.4% and may even be 0%, the content of [D-Glu3] semaglutide does not exceed 0.19%, the contents of [Plus-Gly4] semaglutide, [D-Thr5] semaglutide, and [Plus-Gly16] semaglutide are all 0%, the content of [D-Phe6] semaglutide does not exceed 0.24%, the content of [D-γGlu15] semaglutide does not exceed 0.7%, and the content of [D-γGlu20-3] semaglutide does not exceed 0.29%; the synthesis yield reaches 70% or more; and the maximum single impurity content does not exceed 0.09%, and the total yield is 58% or more. The method greatly reduces costs and facilitates industrial production.[French]
L'invention concerne un procédé de synthèse de sémaglutide. Le procédé comprend principalement : le couplage d'une résine avec un acide aminé protégé et un fragment polypeptidique au moyen d'un procédé de synthèse en phase solide pour obtenir une résine peptidique de sémaglutide, et la réalisation d'un clivage et d'une purification sur la résine peptidique de sémaglutide pour obtenir du sémaglutide, le fragment comprenant Gly29-Arg30, R1-Lys[AEEA-AEEA-γGlu(OR2)-C18-R3]-OH, Glu15-Gly16, Thr5-Phe6 et His1-Aib2-Glu3-Gly4. Le procédé évite efficacement l'apparition de réactions secondaires DKP, augmente le taux de gain de poids de résine à 98% ou plus, améliore le problème de couplage difficile provoqué par des feuilles β, et évite efficacement la génération d'impuretés. Dans le peptide brut, la teneur en [D-His1] sémaglutide ne dépasse pas 0,4% et peut même être 0%, la teneur en [D-Glu3] sémaglutide ne dépasse pas 0,19%, les teneurs en [Plus-Gly4] sémaglutide, [D-Thr5] sémaglutide, et [Plus-Gly16] sémaglutide sont toutes 0%, la teneur en [D-Phe6] sémaglutide ne dépasse pas 0,24%, la teneur en [D-γGlu15] sémaglutide ne dépasse pas 0,7%, et la teneur en [D-γGlu20-3] sémaglutide ne dépasse pas 0,29% ; le rendement de synthèse atteint 70% ou plus ; et la teneur maximale en impuretés uniques ne dépasse pas 0,09%, et le rendement total est de 58% ou plus. Le procédé réduit considérablement les coûts et facilite la production industrielle.[Chinese]
提供了一种司美格鲁肽的合成方法，主要包括：通过固相合成法，将树脂与保护氨基酸及多肽片段进行偶联，得到司美格鲁肽肽树脂，经裂解、纯化得到司美格鲁肽；所述片段包括Gly29-Arg30，R1-Lys[AEEA-AEEA-γGlu(OR2)-C18-R3]-OH，Glu15-Gly16，Thr5-Phe6，His1-Aib2-Glu3-Gly4。有效避免了DKP副反应的发生，提高树脂增重率，达到98％以上；改善了β-折叠导致困难偶联问题，有效避免杂质的生成，粗肽中：[D-His1]司美格鲁肽含量不超过0.4％，甚至含量为0％；[D-Glu3]司美格鲁肽含量不超过0.19％，[Plus-Gly4]司美格鲁肽、[D-Thr5]司美格鲁肽、[Plus-Gly16]司美格鲁肽含量均为0％，[D-Phe6]司美格鲁肽含量不超过0.24％，[D-γGlu15]司美格鲁肽含量不超过0.7％，[D-γGlu20-3]司美格鲁肽含量不超过0.29％；合成收率达到70％以上；最大单杂含量不超过0.09％，总收率58％以上。大大降低成本，有利于工业化生产。