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【结 构 式】 
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【药物名称】Tosufloxacin tosilate, TN-3262a, T-3262a, T-3262, Tosuxacin, Ozex 【化学名称】(±)-7-(3-Amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid p-toluenesulfonate monohydrate 【CA登记号】115964-29-9, 107097-79-0 (free base), 108138-46-1 (free base, anhydrous) 【 分 子 式 】C26H25F3N4O7S 【 分 子 量 】594.57095 |
【开发单位】Toyama (Originator), Abbott (Licensee), Dong-A (Licensee), Nidek (Licensee), Otsuka (Comarketer) 【药理作用】Antibacterial Drugs, Antibacterial Ophthalmic Drugs, ANTIINFECTIVE THERAPY, Ocular Antiinflammatory and Antiinfective Agents, OCULAR MEDICATIONS, Ophthalmic Drugs, DNA Gyrase Inhibitors, DNA Topoisomerase IV Inhibitors, Naphthyridines |
合成路线1
Ethyl 7-chloro-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylate (I) is reacted with 3-aminopyrrolidine dihydrochloride (II), and then the resulting mixture is reacted with potassium hydroxide and p-toluenesulfonic acid monohydrate in order to obtain (rac)-7-(3-amino-1-pyrrolidinyl)-6-fluoro-1-(2,4-difluorophenyl)- 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid p-toluenesulfonate hydrate.
| 【1】 Soejima, R.; Shimada, K.; TOSUFLOXACIN TOSYLATE < Prop INNM >. Drugs Fut 1989, 14, 6, 536. |
| 【2】 Kokei, T.; et al.; Chemical structure and physicochemical properties of (rac)-7-(3-amino-1-pyrrolidinyl)-6-fluoro-1-(2,4-difluorophenyl)-1,4- dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid p-toluensulfonate hydrate (T-3262). Iyakuhin Kenkyu 1988, 19, 682. |
| 【3】 Narita, H.; et al.; Pyridonecarboxylic acids as antibacterial agents IV. Yakugaku Zasshi 1986, 106, 795. |
| 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) | 15230 | ethyl 7-chloro-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylate | C17H10ClF3N2O3 | 详情 | 详情 | |
| (II) | 20938 | 3-pyrrolidinamine; 3-pyrrolidinylamine | C4H10N2 | 详情 | 详情 | |
| (III) | 20939 | ethyl 7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylate | C21H19F3N4O3 | 详情 | 详情 |