CAS: 182349-12-8; 8-Chloro-11-(1-((5-Methylpyridin-3-yl)Methyl)Piperidin-4-Ylidene)-6,11-Dihydro-5H-Benzo[5,6]Cyclohepta[1,2-B]Pyridine Fumarate

3,5-二甲基吡啶置于4-二甲氨基吡啶,N-溴代丁二酰亚胺(Nbs),三乙胺体系中,用 四氯化碳 用作溶剂,化学反应 0.83H,反应生成富马酸卢帕他定
参考文献:一种采用微通道反应装置制备富马酸卢帕他 定的方法
标题:一种采用微通道反应装置制备富马酸卢帕他 定的方法
摘要:本发明公开了一种采用微通道反应装置制备富马酸卢帕他定的方法,在合成富马酸卢帕他定的已知路径上对工艺进行了优化,利用微通道反应装置,反应时间大大缩短,高通量,产品质量稳定,且连续性强有利于连续放大生产,操作简单,安全性高,易于分离,可以有效克服传统合成路径的缺点,显著地提高了产率,达到90%.本发明生产过程中制备的地氯雷他定连续分离,连续分液,溶液直接投入下一步反应,得到卢帕他定,并不会降低产率,简化了操作.

专利信息

专利号:US-6803468-B2
优先权日:2000-08-29
标 题 :Process for the synthesis of n-(5-methylnicontinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine
发明人：KUMAR YATENDRA; PRASAD MOHAN; SINGH SHAILENDRA KUMAR
权利人:RANBAXY LAB LTD
摘要:The present invention relates to an improved and industrially advantageous process for the preparation of N-(5-methylnicotinoyl)-4-hydroxypiperidine of Formula I, as shown in the accompanied drawings. This compound is a key intermediate for the synthesis of rupatadine, a potent dual antagonist of histamine and platelet-activating factor (PAF).

专利号:US-2004044216-A1
优先权日:2000-08-29
标题 :Process for the synthesis of n-(5-methylnicotinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine

专利号:WO-0218366-A1
优先权日:2000-08-29
标题 :Process for the synthesis of n-(5-methylnicotinoyl)-4-hydroxypiperidine, a key intermediate of rupatadine

专利号:CN-105510496-B
优先权日:2015-11-25
标题 :The assay method of DMF residuals in a kind of Rupatadine fumarate bulk drug synthesis technique

专利号:CN-105510496-A
优先权日:2015-11-25
标 题:A method for the determination of DMF residues in the synthesis process of rupatadine fumarate bulk drug

专利号:CN-103804357-A
优先权日:2014-01-02
标 题 :A kind of rupatadine fumarate compound, its synthesis method and its pharmaceutical composition