A method for synthesizing an amanita mushroom alkaloid intermediate

Compound 3 was successfully synthesized by reacting compound 2 and compound 1 at low temperature in an organic solvent, using a specific peptide coupling agent and base, combined with simple extraction and column chromatography techniques. This solved the problems of high conversion rate and high purity of compound 3, making it suitable for industrial applications.

CN122145559APending Publication Date: 2026-06-05SHANGHAI HAOYUAN MEDCHEMEXPRESS CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI HAOYUAN MEDCHEMEXPRESS CO LTD
Filing Date
2024-12-03
Publication Date
2026-06-05

AI Technical Summary

Technical Problem

There is a lack of an economical, fast, easy-to-operate, simple-to-post-process, and high-conversion method for synthesizing compound 3 in the existing technology.

Method used

Compound 2 was reacted with compound 1 in an organic solvent in the presence of a peptide coupling agent and an organic base. HOAT and EDCI were preferably used as peptide coupling agents and NMM as the base. The reaction was carried out under low temperature conditions. Post-treatment was performed by ice-water extraction and methyl tert-butyl ether extraction, combined with simple column chromatography.

Benefits of technology

High conversion rate, low isomer impurity content and high purity of compound 3 were achieved, making it suitable for industrial production. This solved the synthesis problem of compound 3 and provided a liquid-phase, industrially scalable method.

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Abstract

The application belongs to the technical field of medicine and chemistry, and particularly relates to a synthesis method of an amanita intermediate, which comprises the following steps: step 1: reacting compound 2 with compound 1 in the presence of an organic solvent, a peptide coupling agent and an organic base to obtain compound 3. The application is aimed at the obvious disadvantages of the preparation method of amanita in the traditional process, such as low reaction purity, complicated post-treatment and the process that cannot be used for large-scale production. The application improves the process of the important fragment, effectively improves the control purity in the reaction by adjusting the reaction reagent and condition control, avoids racemization and simplifies the post-treatment process. The production method of the application is more suitable for industrial large-scale production, is helpful for saving cost, improving reaction efficiency, product yield and purity.
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