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【结 构 式】 
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【药物名称】710723-S 【化学名称】N-[(1-Ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-(N-methylmethanesulfonamido)benzamide 【CA登记号】90763-18-1 【 分 子 式 】C17H27N3O4S 【 分 子 量 】369.48644 |
【开发单位】Shionogi (Originator) 【药理作用】Antipsychotic Drugs, PSYCHOPHARMACOLOGIC DRUGS |
合成路线1
5-(N-Methylmethanesulfonamido)benzoic acid (I) is treated with thionyl chloride and 2-amino-methyl-1-ethyl-pyrrolidine to give title compound.
| 【1】 Ogata, M.; Matsumoto, H.; Kida, S.; Shiomi, T.; Eigyo, M.; Hirose, K.; Synthesis and neuroleptic activity of N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-sulfonamidobenzamide s. J Med Chem 1984, 27, 9, 1137. |
| 【2】 Ogata, M.; 710723-S. Drugs Fut 1985, 10, 9, 758. |
合成路线2
2-Methoxy-5-(N-methylmethanesulfonamido)-N-tetrahydrofurfurylbenzamide (II), which is prepared from (I) and tetrahydrofurfurylamine, is treated with SOCl2 in dichloroethane to give the dichloro compound (III). Treatment of (III) with EtNH2 gives title compound.
| 【1】 Masaru, O.; Hiroshi, M. (Shionogi & Co. Ltd.); Meta-sulfonamido-benzamides. DE 2803651; ES 466366; FR 2378758; GB 1557019; US 4328155; US 4328344; US 4330472; US 4350635; US 4351770; US 44313663 . |
| 【2】 Ogata, M.; 710723-S. Drugs Fut 1985, 10, 9, 758. |
| 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) | 27331 | 2-methoxy-5-[methyl(methylsulfonyl)amino]benzoic acid | C10H13NO5S | 详情 | 详情 | |
| (II) | 27333 | 2-methoxy-5-[methyl(methylsulfonyl)amino]-N-(tetrahydro-3-furanylmethyl)benzamide | C15H22N2O5S | 详情 | 详情 | |
| (III) | 27334 | N-(2,5-dichloropentyl)-2-methoxy-5-[methyl(methylsulfonyl)amino]benzamide | C15H22Cl2N2O4S | 详情 | 详情 | |
| (IV) | 27335 | Tetrahydro-2-furanylmethanamine; Tetrahydrofurfurylamine | 4795-29-3 | C5H11NO | 详情 | 详情 |
| (V) | 10928 | Ethanamine | 75-04-7 | C2H7N | 详情 | 详情 |
Extended Information