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【结 构 式】 
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【药物名称】Tinazoline hydrohloride, C-7996B-Go, Varsyl 【化学名称】3-(2-Imidazolin-2-ylthio)indole hydrochloride 【CA登记号】55107-60-3, 62882-99-9 (free base) 【 分 子 式 】C11H12ClN3S 【 分 子 量 】253.75539 |
【开发单位】Novartis (Originator) 【药理作用】Nasal Decongestants, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders |
合成路线1
Oxidative coupling of indole (I) and ethylenethiourea (II) with iodine and potassium iodide affords the hydroiodide salt (III) in 89% yield. The hydroiodide salt is converted into the hydrochloride salt on an ion exchange column or through the base.
| 【1】 Shah, .K.; Nagarajan, K.; Arya, V.P.; Parthasarathy, T.N.; Shenoy, S.J.; Kulkarni, Y.S.; Derivatives of 3-mercaptoindole - Synthesis of a potent vasoconstrictor, 3-(2-imidazolin-2-ylthio)indole(tinazole). Indian J Med 1981, 20B, 672-679. |
| 【2】 Arya, V.P.; Nagarajan, K. (Novartis Corp.); Condensed pyrrole mercapto compounds. DE 2427207; FR 2233047; JP 50035160; US 3954757 . |
| 【3】 Arya, V.P.; Tinazoline hydrochloride. Drugs Fut 1982, 7, 5, 325. |
| 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) | 15292 | Indole; 1H-indole | 120-72-9 | C8H7N | 详情 | 详情 |
| (II) | 31949 | Ethylenethiourea; 2-Imidazolidinethione | 96-45-7 | C3H6N2S | 详情 | 详情 |
| (III) | 31950 | 4,5-dihydro-1H-imidazol-2-yl 1H-indol-3-yl sulfide; 3-(4,5-dihydro-1H-imidazol-2-ylsulfanyl)-1H-indole | C11H11N3S | 详情 | 详情 | |
| (IV) | 31950 | 4,5-dihydro-1H-imidazol-2-yl 1H-indol-3-yl sulfide; 3-(4,5-dihydro-1H-imidazol-2-ylsulfanyl)-1H-indole | C11H11N3S | 详情 | 详情 |
Extended Information