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【结 构 式】 
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【药物名称】D-11208 【化学名称】N-[2-Amino-6-(4-trifluoromethylbenzylamino)pyridin-3-yl]carbamic acid ethyl ester hydrochloride 【CA登记号】91940-99-7 【 分 子 式 】C16H18ClF3N4O2 【 分 子 量 】390.79566 |
【开发单位】Degussa (Originator) 【药理作用】Antiepileptic Drugs, NEUROLOGIC DRUGS |
合成路线1
D-11208 is obtained in a five step synthesis: 2,6-Dichloro-3-nitropyridine (I) reacts with ammonia to give 2-amino-3-nitro-6-chloropyridine (II). Subsequent condensation with 4-trifluoromethyl benzylamine (III) yields 2-amino-3-nitro-6-(4-trifluoromethyl)aminopyridine (IV). Hydrogenation with Raney Nickel as catalyst and reaction with ethyl chloroformiate yields D-11208.
| 【1】 Bebengurg, W.; Engek, J.; Heese, J.; Thiele, K. (Degussa AG); 2-Amino-3-acylamino-6-benzylaminopyridine derivatives having antiepileptic action. DE 3337593 . |
| 【2】 Engel, J.; Molliere, M.; Emig, P.; Szelenyi, I.; D-11208. Drugs Fut 1988, 13, 9, 817. |
| 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) | 13574 | 2,6-Dichloro-3-nitropyridine | 16013-85-7 | C5H2Cl2N2O2 | 详情 | 详情 |
| (II) | 13575 | 6-Chloro-3-nitro-2-pyridinamine; 2-Amino-6-chloro-3-nitropyridine; 6-Chloro-3-nitro-2-pyridinylamine | 27048-04-0 | C5H4ClN3O2 | 详情 | 详情 |
| (III) | 21925 | [4-(trifluoromethyl)phenyl]methanamine; 4-(trifluoromethyl)benzylamine | 3300-51-4 | C8H8F3N | 详情 | 详情 |
| (IV) | 23270 | N-(6-amino-5-nitro-2-pyridinyl)-N-[4-(trifluoromethyl)benzyl]amine; 3-nitro-N(6)-[4-(trifluoromethyl)benzyl]-2,6-pyridinediamine | C13H11F3N4O2 | 详情 | 详情 | |
| (V) | 23271 | 2-amino-6-[[4-(trifluoromethyl)benzyl]amino]-3-pyridinylamine; N(6)-[4-(trifluoromethyl)benzyl]-2,3,6-pyridinetriamine | C13H13F3N4 | 详情 | 详情 |
Extended Information