盐酸西那卡塞的合成工艺研究
Synthesis Process of Cinacalcet Hydrochloride
DOI: 10.12677/HJMCe.2014.21001, PDF,  被引量   
作者: 卞学国：南京医工医药有限公司，南京；王均伟：南京医工医药有限公司，南京;中国药科大学药物化学教研室，南京；朱启华, 徐云根：中国药科大学药物化学教研室，南京
关键词: 盐酸西那卡塞；合成；工艺研究；Cinacalcet Hydrochloride; Synthesis; Process Research
摘要: 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。
Abstract: 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.
文章引用：卞学国, 王均伟, 朱启华, 徐云根. 盐酸西那卡塞的合成工艺研究[J]. 药物化学, 2014, 2(1): 1-5. https://dx.doi.org/10.12677/HJMCe.2014.21001

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