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【结 构 式】

【药物名称】SIB-1553A

【化学名称】(±)-2-[2-(4-Hydroxyphenylsulfanyl)ethyl]-1-methylpyrrolidine hydrochloride

【CA登记号】191611-76-4 (free base)

【 分 子 式 】C13H20ClNOS

【 分 子 量 】273.82745

【开发单位】Merck & Co. (Originator)

【药理作用】Alzheimer's Dementia, Treatment of , Cognition Disorders, Treatment of, NEUROLOGIC DRUGS, Nicotinic Receptor Agonists

合成路线1

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 .
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) 22546 4-sulfanylphenol 637-89-8 C6H6OS 详情 详情
(II) 30816 2-(2-chloroethyl)-1-methylpyrrolidine C7H14ClN 详情 详情
Extended Information