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Rivastigmine tartrate, ENA-713, SDZ-212-713, SDZ-ENA-713, Exelon MR, Exelon TDS, Prometax, Exelon

酒石酸卡巴拉汀 利凡斯的明 Chemical Name: (S)-N-Ethyl-N-methylcarbamic acid 3-[1-(dimethylamino)ethyl]phenyl ester hydrogen(R,R)-tartrate
CAS No. 129101-54-8, 123441-03-2 (free base)
项目整合开发状态: Launched-1997
项目研究机构: Novartis (Originator), Esteve (Licensee)
合成路线:Reaction of 3-[1-(dimethylamino)ethyl]phenol (I) with N-ethyl-N-methylcarbamoyl chloride (II) and sodium hydride in tetrahydrofuran gives racemic N-ethyl-N-methylcarbamic acid 3-[1-(dimethylamino)ethyl]phenyl ester (III),which is resolved by recrystallization with (+)-D-di-O,O'-(p-toluoyl)tartaric acid in methanol followed by treatment with base.
📌 参考资料/链接:
参考文献标题:Phenylcarbamate
文献作者:Enz,A.(Novartis Deutschland GmbH)
参考来源:AU 8812554; BE 1001467; CH 675720; DE 3805744; FR 2611707; GB 2203040; JP 1988238054; JP 1997118617; JP 1997165362

📄 详细内容


合成路线:Reaction of 3-[1-(dimethylamino)ethyl]phenol (I) with N-ethyl-N-methylcarbamoyl chloride (II) and sodium hydride in tetrahydrofuran gives racemic N-ethyl-N-methylcarbamic acid 3-[1-(dimethylamino)ethyl]phenyl ester (III),which is resolved by recrystallization with (+)-D-di-O,O'-(p-toluoyl)tartaric acid in methanol followed by treatment with base.

参考文献标题:SDZ-ENA-713
文献作者:Rabasseda,X.; Castar,J.; Prous,J.
参考来源:Drugs Fut 1994,19(7),656


合成路线:Reaction of 3-[1-(dimethylamino)ethyl]phenol (I) with N-ethyl-N-methylcarbamoyl chloride (II) and sodium hydride in tetrahydrofuran gives racemic N-ethyl-N-methylcarbamic acid 3-[1-(dimethylamino)ethyl]phenyl ester (III),which is resolved by recrystallization with (+)-D-di-O,O'-(p-toluoyl)tartaric acid in methanol followed by treatment with base.
参考文献标题:Cyclic phenyl-carbamates of the myotin-type and their action on acetylcholinesterase
文献作者:Amstutz,R.; Walkinshaw,M.; Marzi,M.; Enz,A.; Boelsterli,J.
参考来源:Helv Chim Acta 1990,73739-53


产品链接: CAS No. 129101-54-8››

产品链接: CAS No.123441-03-2››