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【结 构 式】 
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【分子编号】12966 【品名】3-[1-(dimethylamino)ethyl]phenyl ethyl(methyl)carbamate 【CA登记号】 |
【 分 子 式 】C14H22N2O2 【 分 子 量 】250.34096 【元素组成】C 67.17% H 8.86% N 11.19% O 12.78% |
与该中间体有关的原料药合成路线共 2 条
合成路线1
该中间体在本合成路线中的序号：(III)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.
| 【1】 Enz, A. (Novartis Deutschland GmbH); Phenylcarbamate. AU 8812554; BE 1001467; CH 675720; DE 3805744; FR 2611707; GB 2203040; JP 1988238054; JP 1997118617; JP 1997165362 . |
| 【2】 Amstutz, R.; Walkinshaw, M.; Marzi, M.; Enz, A.; Boelsterli, J.; Cyclic phenyl-carbamates of the myotin-type and their action on acetylcholinesterase. Helv Chim Acta 1990, 73, 739-53. |
| 【3】 Rabasseda, X.; Castaner, J.; Prous, J.; SDZ-ENA-713. Drugs Fut 1994, 19, 7, 656. |
合成路线2
该中间体在本合成路线中的序号：(III)
| 【1】 Jaweed M, Siddiqui M, Upadhye BK, et al. 2007. Process for preparing enantiomerically pure rivastigmine. W0 2007026373 |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 25331 | 3-hydroxyacetophenone; 1-(3-hydroxyphenyl)-1-ethanone | 121-71-1 | C8H8O2 | 详情 | 详情 |
| (II) | 12964 | 3-[1-(Dimethylamino)ethyl]phenol | C10H15NO | 详情 | 详情 | |
| (III) | 12966 | 3-[1-(dimethylamino)ethyl]phenyl ethyl(methyl)carbamate | C14H22N2O2 | 详情 | 详情 | |
| (IV) | 66627 | 2,3-bis((4-methylbenzoyl)oxy)succinic acid mixtures | C20H18O8 | 详情 | 详情 |
Extended Information