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【结 构 式】 
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【药物名称】TA-5707 【化学名称】6-Methyl-N-1H-tetrazol-5-yl-2-pyridinecarboxamide monosodium salt 【CA登记号】83282-09-1, 83282-08-0 (free acid) 【 分 子 式 】C8H7N6NaO 【 分 子 量 】226.17439 |
【开发单位】Tanabe Seiyaku (Originator) 【药理作用】Antiallergy/Antiasthmatic Drugs, Asthma Therapy, RESPIRATORY DRUGS, Mediator Release Inhibitors |
合成路线1
The reaction of 6-methylpyridine-2-carboxylic acid (I) with refluxing SOCl2 gives 6-methylpyridine-2-carbonyl chloride (II), which is condensed with 5-aminotetrazole (III) by means of triethylamine in hot DMF.
| 【1】 Takeda, M.; Honma, Y.; Tsuzurahara, K.; 2-Pyridinecarboxamide derivatives compositions containing same and method of using same. EP 0053789; ES 8303398; JP 1482289C; JP 57095984; US 4404214 . |
| 【2】 Takeda, M.; Sekine, Y.; Ono, Y.; Hashiyama, T.; Honma, Y.; Tsuzurahara, K.; Hanamoto, K.; Antiallergic agents. 3. N-(1H-Tetrazol-5-yl)-2-pyridinecarboxamides. J Med Chem 1984, 27, 2, 125-128. |
| 【3】 Serradell, M.N.; Castaner, J.; TA-5707. Drugs Fut 1984, 9, 7, 527. |
| 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) | 30380 | 6-methyl-2-pyridinecarboxylic acid | 934-60-1 | C7H7NO2 | 详情 | 详情 |
| (II) | 34352 | 6-methyl-2-pyridinecarbonyl chloride | C7H6ClNO | 详情 | 详情 | |
| (III) | 14092 | 1H-1,2,3,4-Tetraazol-5-ylamine; 1H-Tetrazol-5-amine; 1H-1,2,3,4-Tetraazol-5-amine; 5-Amino-1H-1,2,3,4-tetrazole | 4418-61-5 | CH3N5 | 详情 | 详情 |
Extended Information