aliskiren的合成

Q4 Pharmacology, Toxicology and Pharmaceutics

中国药科大学学报 Pub Date : 2011-01-01 DOI:10.1055/s-0034-1380902

Wu Xiaoming

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引用次数: 0

摘要

本文介绍了一种制备阿利斯基仑的实用工艺。通过化学拆分制备手性构建块1和2，经过5步会聚合成得到aliskiren，总收率为15.6%。通过熔点、核磁共振和质谱对中间体和目标化合物进行了表征。聚类合成工艺产率合理，操作简便，立体选择性高，且只需一次色谱纯化，适合大规模生产。

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Synthesis of aliskiren

This paper describes a practical process for the preparation of aliskiren.Chiral building blocks 1 and 2 were prepared by chemical resolution,and a following five-step convergent synthesis led to aliskiren with an overall yield of 15.6%.The intermediates and the target compound were characterized by melting points,NMR and MS.The convergent synthetic process of aliskiren highlights reasonable yields,ease of operation,high stereoselectivity as well as only one chromatographic purification,and thus should be amenable to large-scale production.

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来源期刊

中国药科大学学报 Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

0.40

自引率

0.00%

发文量

6190

期刊介绍：