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【结 构 式】 
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【药物名称】Mopidralazine, MDL-899 【化学名称】N-(2,5-Dimethyl-1H-pyrrol-1-yl)-6-(4-morpholinyl)-3-pyridazinamine 【CA登记号】75841-82-6, 75841-84-8 (HCl), 77510-09-9 (sulfate) 【 分 子 式 】C14H19N5O 【 分 子 量 】273.34043 |
【开发单位】Lepetit (Originator) 【药理作用】CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Vasodilators |
合成路线1
The starting compound is 3,6-dichloropyridazine (I), which is reacted with morpholine (II) in a suitable solvent to give 3-morpholino-6-chloropyridazine (III). This, upon reaction with hydrazine hydrate as solvent, gives the hydrazine derivative (IV), which by reaction with acetonylacetone (V) in acetic acid yields directly the title compound. [14C]-Labeled compound is synthesized by a microscale procedure with 45% chemical yield and 98% radiochemical purity.
| 【1】 Assandri, A.; et al.; Pharmacokinetics of a new antihypertensive pyrrolyl pyridazinamine (MDL-899) in the rat and the dog. Arzneim-Forsch Drug Res 1985, 35, 2, 508. |
| 【2】 Koch, H.; Mopidralazine. Drugs Fut 1985, 10, 8, 634. |
| 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) | 11292 | 3,6-Dichloropyridazine | 141-30-0 | C4H2Cl2N2 | 详情 | 详情 |
| (II) | 10308 | 2-Chloronicotinonitrile; 2-Chloro-3-cyanopyridine | 6602-54-6 | C6H3ClN2 | 详情 | 详情 |
| (III) | 24846 | 4-(6-chloro-3-pyridazinyl)morpholine | C8H10ClN3O | 详情 | 详情 | |
| (IV) | 24847 | 4-(6-hydrazino-3-pyridazinyl)morpholine | C8H13N5O | 详情 | 详情 | |
| (V) | 24848 | acetonyl acetone;1,2-Diacetylethane;a,b-Diacetylethane;2,5-Diketohexane;Diacetonyl;Acetonylacetone;2,5-Dioxohexane;2,5-hexanedione | 110-13-4 | C6H10O2 | 详情 | 详情 |