Synthesis method of semaglutide
The synthesis of somaglutide by one pot method has solved the problems of many impurities, low purity and low yield in the prior art, and achieved high yield and high purity somaglutide synthesis, which is suitable for industrial production.
CN120424191APending Publication Date: 2025-08-05SINOPEP ALLSINO BIOPHARMACEUTICAL CO LTD +1
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Patent Information
- Application Number
- CN202510573906.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-04-30
- Publication Date
- 2025-08-05
AI Technical Summary
Technical Problem
The existing somaglutide synthesis methods have problems such as many impurities, low purity, low yield, cumbersome operation steps and high cost.
Method used
The one-pot synthesis method was adopted, and the peptide was dispersed in the liquid and the alkali catalyst was added to react with Oct-γ-Glu-AEEA-AEEA-activated ester solution, followed by the addition of activated Fmoc-His-Aib-OH and OSu palmitate for the blocking reaction. Finally, the Fmoc removal reagent was used and diluted to avoid the operational inconvenience and yield loss caused by the acid precipitation in the middle.
Benefits of technology
The high yield (82.30%) and high purity (84.33%) of somaglutide are achieved, and the operation steps are simplified, which is conducive to industrial production.
✦ Generated by Eureka AI based on patent content.
Abstract
The invention belongs to the field of polypeptide drug synthesis, and particularly relates to a synthesis method of semaglutide. The synthesis method of the semaglutide provided by the invention comprises the following steps: dispersing peptide in liquid, adding a base catalyst and an Oct-gamma-Glu-AEA-AEA-activated ester solution to react, adding activated Fmoc-His-Aib-OH into the obtained reaction liquid 1, and reacting to obtain a reaction liquid 2; and adding a palmitic acid OSu ester solution into the reaction solution 2 to carry out an end-capping reaction, adding an Fmoc removal reagent into the obtained end-capping reaction solution to carry out a reaction, and adding water to dilute to obtain the semaglutide. Through a one-pot feeding mode, operation inconvenience and yield loss caused by midway acid regulation and sedimentation are avoided, and the dipeptide feeding amount and purification difficulty are reduced by adopting an end capping mode. The synthesis method disclosed by the invention is simple to operate, the obtained semaglutide is high in yield, the semaglutide with higher purity can be obtained without purification, and industrial large-scale production is facilitated.
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