Preparation method of ranolazine

The Fmoc-Cl monosubstituted piperazine method simplifies the ranolazine synthesis process, solving the problems of long synthesis routes and numerous by-products in existing technologies, and achieving efficient and low-cost ranolazine production.

CN120623124BActive Publication Date: 2025-10-28福安药业集团重庆博圣制药有限公司
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Patent Information

Application Number
CN202511113290.5
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2025-08-11
Publication Date
2025-10-28
Estimated Expiration
2045-08-11

AI Technical Summary

Technical Problem

Existing methods for synthesizing ranolazine suffer from drawbacks such as long synthetic routes, numerous byproducts, and significant environmental impact, making it difficult to achieve efficient and low-cost industrial production.

Method used

The Fmoc-Cl monosubstituted piperazine method involves reacting N-Fmoc-piperazine with 2-chloro-N-(2,6-dimethyl)acetamide and l-(2-methoxyphenoxy)-2,3-epoxypropane under alkaline conditions, thus avoiding the formation of disubstituted piperazine products, simplifying the process steps, and improving purity and conversion rate.

Benefits of technology

It effectively reduces the formation of piperazine disubstituted products, lowers raw material costs, improves conversion rate and purity, shortens the production cycle, reduces solvent usage, and is suitable for large-scale production.

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Abstract

This invention belongs to the field of pharmaceutical synthesis technology, specifically relating to a novel method for preparing ranolazine. The invention employs Fmoc-Cl to unilaterally protect piperazine, preparing N-Fmoc-piperazine; the obtained N-Fmoc-piperazine reacts with 2-chloro-N-(2,6-dimethylphenyl)acetamide to prepare N-Fmoc-N-(2,6-dimethylphenyl)-1-piperazineacetamide, which is then deprotected under alkaline conditions and reacted with 1-(2-methoxyphenoxy)-2,3-epoxypropane to prepare crude ranolazine; the crude product is recrystallized to obtain the final product. The 1-(2-methoxyphenoxy)-2,3-epoxypropane reaction solution is prepared by reacting o-methoxyphenol, epichlorohydrin, and alkali in water. This method effectively avoids the formation of disubstituted piperazine derivatives, significantly reduces the amount of piperazine used, and features a short production cycle, low cost, and suitability for industrial production.
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