右兰索拉唑的合成工艺研究 |
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引用本文: | 于晓玲,郑志超,梅林雨,罗振福,孙有光.右兰索拉唑的合成工艺研究[J].现代药物与临床,2013,28(5):661-664. |
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作者姓名: | 于晓玲 郑志超 梅林雨 罗振福 孙有光 |
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作者单位: | 天津理工大学 化学化工学院,天津 300384;天津药物研究院 化学制药部,天津 300193;天津理工大学 化学化工学院,天津 300384 |
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基金项目: | 天津市应用基础与前沿技术研究计划资助项目(11JCZDJC24400) |
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摘 要: | 目的 对右兰索拉唑的合成工艺进行研究。方法 以4-氯-2,3-二甲基吡啶-N-氧化物为起始原料,经酰化、水解、氯代、取代反应得到兰索拉唑硫醚,再进行不对称氧化、取代反应获得右兰索拉唑。结果 合成右兰索拉唑对映体过量值(ee值)为99.5%,总收率为21.6%。结论 改进后的工艺成本低、操作方法简单、后处理容易、收率高、产物纯度高、可用于工业放大生产。
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关 键 词: | 右兰索拉唑 不对称氧化 合成 |
Synthesis technology of dexlansoprazole |
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Abstract: | Objective To study the synthetic technology of dexlansoprazole. Methods Using 4-chloro-2,3-dimethy-pyridine- N-oxide as the starting material, dexlansoprazole was obtained after a series of chemical reactions including acylation, hydrolysis, chlorination, and substitution reaction to give dexlansoprazole sulfide, then asymmetric oxidation and substitution were carried out. Results The total yield with 99.5% enantiomeric excess of dexlansoprazole was up to 21.6%. Conclusion The improved procedure has the advantages of low cost, simple operating procedure, easy post-processing and fine yield. The purity of the product is high and can be scaled up to industrial production. |
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Keywords: | dexlansoprazole asymmetric oxidation synthesis |
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