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药物化学
Vol. 2 No. 1 (February 2014)
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盐酸西那卡塞的合成工艺研究
Synthesis Process of Cinacalcet Hydrochloride
DOI:
10.12677/HJMCe.2014.21001
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被引量
下载: 3,670
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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.
http://dx.doi.org/10.12677/HJMCe.2014.21001
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