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【结 构 式】 
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【药物名称】Emorfazone, M-73101, Pentoil 【化学名称】4-Ethoxy-2-methyl-5-(4-morpholinyl)-3(2H)-pyridazinone 【CA登记号】38957-41-4 【 分 子 式 】C11H17N3O3 【 分 子 量 】239.27644 |
【开发单位】Morishita (Originator) 【药理作用】Non-Steroidal Antiinflammatory Drugs |
合成路线1
Compound can be prepared in two different ways: 1) The condensation of 4,5-dichloro-2-methyl-3-(2H)pyridazinone (I) with morpholine (A) in refluxing ethanol gives 2-methyl-4-chloro-5-morpholino-3(2H)-pyridazinone (II), which is then treated with sodium ethoxide in refluxing ethanol. 2) The reaction of 2-methyl-4,6-dichloro-5-morpholino-3(2H)pyridazinone (III) with sodium ethoxide in refluxing ethanol gives 2-methyl-4-ethoxy-5-morpholino-6-chloro-3(2H)-pyridazinone (IV), which is then reduced with H2 over Pd/C in THF.
| 【1】 Satoda, I.; et al.; JP 7224030 . |
| 【2】 Satoda, I.; et al.; 2-Alkyl-4-alkoxy-5-morpholino-3-2H-pyridazinones and their method of preparation. GB 1351569 . |
| 【3】 Satoda, I.; et al.; Verfahren zur Herstellung von 2-Alkyl-4-alkoxy-5-morpholino-3(2H)-pyridazinon. DE 2225218 . |
| 【4】 Kishikawa, T.; Matsuo, T.; JP 7659882 . |
| 【5】 Castaner, J.; Blancafort, P.; M-73101. Drugs Fut 1978, 3, 10, 756. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (A) | 10388 | Morpholine | 110-91-8 | C4H9NO | 详情 | 详情 |
| (I) | 33532 | 4,5-dichloro-2-methyl-3(2H)-pyridazinone | 933-76-6 | C5H4Cl2N2O | 详情 | 详情 |
| (II) | 33533 | 4-chloro-2-methyl-5-(4-morpholinyl)-3(2H)-pyridazinone | C9H12ClN3O2 | 详情 | 详情 | |
| (III) | 33534 | 4,6-dichloro-2-methyl-5-(4-morpholinyl)-3(2H)-pyridazinone | C9H11Cl2N3O2 | 详情 | 详情 | |
| (IV) | 33535 | 6-chloro-4-ethoxy-2-methyl-5-(4-morpholinyl)-3(2H)-pyridazinone | C11H16ClN3O3 | 详情 | 详情 |