Process for the preparation of glp-1 receptor agonist intermediates
By optimizing the preparation process of GLP-1 receptor agonist compound I, using intermediate 3 and stepwise hydrolysis, combined with a specific reducing agent composition, the problems of cumbersome reaction steps and low purity in the prior art were solved, and high-yield and high-purity compound I production was achieved.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- HANGZHOU ZHONGMEI HUADONG PHARMACEUTICAL CO LTD
- Filing Date
- 2022-08-16
- Publication Date
- 2026-06-19
AI Technical Summary
In the existing technology, the preparation of GLP-1 receptor agonist compound I has problems such as complicated reaction steps, easy chiral configuration reversal, low yield and low purity. In particular, during the hydrolysis of ester group and amide bond, the content of isomer impurities is high, which affects the product quality.
By replacing intermediate A with intermediate 3, the preparation method of compound 2 was optimized through stepwise hydrolysis and asymmetric reduction reactions using a specific combination of inorganic base and organic acid. Furthermore, the reducing agent composition MBH(RCOO)3 and zinc borohydride were added during the reduction process of compound 2 to increase steric hindrance and improve selectivity.
It effectively reduced the content of chiral isomers, improved the yield and purity of compound I, made it suitable for industrial production, and significantly improved product quality.
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