Preparation method of topiromilast
By reacting compound 2 and compound 3 under the action of potassium iodide and tert-butanol of hydrogen peroxide, the problem of using highly toxic cyanide reagents and harsh reaction conditions in the existing topilistat synthesis route was solved, and the preparation of topilistat with high yield and high purity was achieved, which was suitable for industrial production.
CN119638668APending Publication Date: 2025-03-18SHANDONG NEW TIME PHARMA CO LTD
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Patent Information
- Application Number
- CN202311194030.6
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2023-09-15
- Publication Date
- 2025-03-18
AI Technical Summary
Technical Problem
The existing topivalst synthesis route uses highly toxic cyanide reagents, with harsh reaction conditions, long process routes, high raw material costs and low yields, making it difficult to be suitable for industrial production.
Method used
Compound 2 and Compound 3 were reacted under the action of potassium iodide and hydrogen peroxide tert-butanol, and topilist was obtained after post-treatment. This method simplifies the process route, reduces the use of cyanide reagents, and is suitable for industrial production.
Benefits of technology
The preparation of topilist with high yield and high purity is achieved, which reduces production costs and simplifies post-treatment operations, and is suitable for industrial production.
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Abstract
The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of topiromilast. The preparation method comprises the following steps: reacting 4-(aminomethyl) pyridine-2-formonitrile and 4-pyridylaldehyde hydrazone serving as raw materials under the action of potassium iodide and tert-butyl hydroperoxide; and performing post-treatment to obtain the target compound topiromilast. The initial raw materials are simple, cheap and easy to obtain, the production cost can be effectively reduced, and introduction of a cyaniding reagent in the synthesis process can be greatly reduced; the yield and the purity of the product are improved, the post-treatment operation is simple, and the method is suitable for industrial production.
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