|
【结 构 式】 
|
【分子编号】30816 【品名】2-(2-chloroethyl)-1-methylpyrrolidine 【CA登记号】 |
【 分 子 式 】C7H14ClN 【 分 子 量 】147.6476 【元素组成】C 56.94% H 9.56% Cl 24.01% N 9.49% |
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)The cyclization of alpha-(p-chlorophenyl)acetophenone-o-carboxylic acid (I) with hydrazine sulfate by means of NaOH in water gives 4-(p-chlorobenzyl)-1-(2H)-phthalazinone (II), which is then condensed with 2-(2-chloroethyl)-N-methylpyrrolidine (III) by means of NaOH in hot water.
| 【1】 Vogelsong, D.; et al.; Basically substituted benzyl phthalazone derivatives acid salts thereof and process for the production thereof. US 3813384 . |
| 【2】 Hillier, K.; Blancafort, P.; Castaner, J.; Serradell, M.N.; Azelastine. Drugs Fut 1980, 5, 3, 123. |
合成路线2
该中间体在本合成路线中的序号：(II)The condensation of 4-hydroxythiophenol (I) with 2-(2-chloroethyl)-1-methylpyrrolidine (II) in the presence of K2CO3 in DMF afforded the title thioether, which was isolated as the hydrochloride salt.
| 【1】 El-Abdellaoul, H.; Holsenback, H.; Vernier, J.-M.; et al.; 4-[[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A): A novel cognitive enhance with selectivity for neuronal nicotinic acetylcholine receptors. J Med Chem 1999, 42, 10, 1684. |
| 【2】 Vernier, J.M.; McDonald, I.A. (SIBIA Neurosciences, Inc.); Novel substd. aryl cpds. useful as modulators of acetylcholine receptors. EP 0874818; JP 2000501080; WO 9719059 . |
Extended Information