|
【结 构 式】 
|
【药物名称】 【化学名称】6-Chloro-5-methyl-N-[6-(2-methylpyridin-3-yloxy)pyridazin-3-yl]indoline-1-carboxamide 【CA登记号】300554-31-8 【 分 子 式 】C20H18ClN5O2 【 分 子 量 】395.85176 |
【开发单位】GlaxoSmithKline (Originator) 【药理作用】Antidepressants, Anxiolytics, Mood Disorders, Treatment of, PSYCHOPHARMACOLOGIC DRUGS, 5-HT2C (5-HT1C) Inverse Agonists |
合成路线1
Condensation between 3-amino-6-chloropyridazine (I) and 3-hydroxy-2-methylpyridine (II) in aqueous NaOH at 175 C under pressure afforded the bisaryl ether (III). The phenyl carbamate (IV) was then prepared by treatment of aminopyridazine (III) with phenyl chloroformate. Finally, coupling of carbamate (IV) with 6-chloro-5-methylindoline (V) yielded the title urea derivative.
| 【1】 Bromidge, S.M.; Davies, S.; Dabbs, S.; et al.; 1-[2-(Heteroaryloxy)heteroaryl]carbamoy]indolines: Novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents. Bioorg Med Chem Lett 2000, 10, 16, 1863. |
| 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) | 43962 | 6-chloro-3-pyridazinamine; 6-chloro-3-pyridazinylamine | 5469-69-2 | C4H4ClN3 | 详情 | 详情 |
| (II) | 29609 | 2-methyl-3-pyridinol | 1121-25-1 | C6H7NO | 详情 | 详情 |
| (III) | 43963 | 6-[(2-methyl-3-pyridinyl)oxy]-3-pyridazinamine; 6-[(2-methyl-3-pyridinyl)oxy]-3-pyridazinylamine | C10H10N4O | 详情 | 详情 | |
| (IV) | 43964 | phenyl 6-[(2-methyl-3-pyridinyl)oxy]-3-pyridazinylcarbamate | C17H14N4O3 | 详情 | 详情 | |
| (V) | 26798 | 6-chloro-5-methylindoline | C9H10ClN | 详情 | 详情 |
Extended Information