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【结 构 式】 
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【药物名称】 【化学名称】2-[1-(2-Phenylethyl)piperidin-2-yl]acetic acid methyl ester 【CA登记号】247259-34-3 【 分 子 式 】C16H23NO2 【 分 子 量 】261.36721 |
【开发单位】Georgia Institute of Technology (Originator), Mercer University (Originator) 【药理作用】Treatment of Cocaine Dependency, TREATMENT OF POISONING, DRUG ABUSE & DEPENDENCY, Treatment of Substance Dependency, Dopamine Reuptake Inhibitors |
合成路线1
2-Pyridyl acetic acid (I) is converted into its methyl ester derivative (II) by means of SOCl2 in MeOH and then vigorously hydrogenated over Pt in MeOH to afford 2-(2-piperidyl)acetic acid methyl (III). Finally, piperidine ester derivative (III) is alkylated on nitrogen with 2-phenylethylbromide (IV) in DMF in the presence of K2CO3.
| 【1】 Dunn, T.; Deutsch, H.M.; Schweri, M.M.; Ye, X.; Synthesis and pharmacology of site-specific cocaine abuse treatment agents: The role of the phenyl group in highly modified methylphenidate analogs as dopamine uptake inhibitors. Med Chem Res 1999, 9, 4, 213. |
| 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) | 44792 | 2-(3-pyridazinyl)acetic acid | C6H6N2O2 | 详情 | 详情 | |
| (II) | 44793 | methyl 2-(3-pyridazinyl)acetate | C7H8N2O2 | 详情 | 详情 | |
| (III) | 44794 | methyl 2-hexahydro-3-pyridazinylacetate | C7H14N2O2 | 详情 | 详情 | |
| (IV) | 20730 | 1-(2-bromoethyl)benzene；1-Bromo-2-phenylethane;(2-Bromoethyl)benzene;Phenethyl bromide | 103-63-9 | C8H9Br | 详情 | 详情 |
Extended Information