Givinostat and a method for its synthesis

By simplifying the synthetic route of givestrap, compound 1 reacts with hydroxylamine hydrochloride to generate compound 2, and compound 3 to the target product requires only 4 steps of reaction, which solves the problems of low yield and cumbersome operation in the prior art and realizes the preparation of givestrap with high yield and low cost.

CN122102955APending Publication Date: 2026-05-29SICHUAN LIRUIZE BIOTECHNOLOGY CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SICHUAN LIRUIZE BIOTECHNOLOGY CO LTD
Filing Date
2026-01-28
Publication Date
2026-05-29

AI Technical Summary

Technical Problem

Existing synthetic routes for gemvestal have low yields and are cumbersome to operate, making it difficult to meet the needs of large-scale production, and impurities are difficult to remove effectively.

Method used

Compound 1 was reacted with hydroxylamine hydrochloride to generate compound 2, and compound 3 was reacted in three steps to synthesize intermediate 6. Finally, it was reacted with compound 2 to generate givestia, which simplified the synthetic route and improved the yield.

Benefits of technology

The yields of compounds 1 to 2 reached over 80%, and the total yield of compound 3 to the target product reached over 40%, simplifying the purification steps and reducing the preparation cost.

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Abstract

The application discloses givinostat and a synthesis method thereof, wherein compound 1 is used for synthesizing compound 2 in step 01; compound 3 is used for synthesizing compound 4 in step 02; compound 4 is used for synthesizing compound 5 in step 03; compound 5 is used for synthesizing compound 6 in step 04; and compound 6 and compound 2 are used for synthesizing givinostat in step 05. After optimization, the yield of compound 1 to compound 2 reaches more than 80 %, raw materials and reagents used in the reaction are cheap and easy to obtain, and the preparation cost is very low; only four steps are needed from compound 3 to the target product, the route is short, and the operation is simple; and after optimization, the total yield of compound 3 to the target product reaches more than 40 %, the yield is high, and the preparation cost is significantly reduced.
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Citation Information

Patent Citations

  • Compounds with Anti-inflammatory and immunosuppressive activities

    WO1997043251A1

  • Monohydrate hydrochloride of the 4-hydroxycarbamoyl-phenyl)-carbamic acid (6-diethylaminomethyl-naphtalen-2-YL) ester

    WO2004065355A1