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盐酸西那卡塞的合成工艺研究
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Abstract:
目的：确定一条适合工业化生产的盐酸西那卡塞的合成工艺。方法：以1-萘乙酮为起始原料，经Leuckart- Wallch反应、水解、手性拆分、缩合、还原、成盐6步反应合成盐酸西那卡塞。结果：通过工艺改进，简化了操作过程，提高了安全性，降低了生产成本，总收率14.38%(此合成路线总收率未经文献报道)，纯度99.9%。结论：本方法条件温和，操作简单，成本低，收率高，适合大规模生产。
Objective: In order to get a suitable process of cinacalcet hydrochloride for industrial production. Methods: Cinacalcet hydrochloride was synthesized from 1-acetonaphthone via six steps, including Leuckart-Wallch reaction, hydrolysis, chiral resolution, condensation, reduction and finally salification. Results: Through improvement, we simplified the operations, improved the safety of the process and reduced the costs. The overall yield was 14.38% (The overall yield of this synthetic route was unreported) with a purity of 99.9%. Conclusion: This synthetic process is of mild conditions, easy operation, low cost and high yield, and is suitable for large-scale production.
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