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【结 构 式】 
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【药物名称】Moxonidine hydrochloride hydrate, LY-326869, BE-5895, BDF-5895, Norcynt, Nucynt, Moxon, Normoxin, Physiotens, Lomox, Cynt 【化学名称】4-Chloro-5-(2-imidazolin-2-ylamino)-6-methoxy-2-methylpyrimidine hydrochloride hydrate 【CA登记号】75438-57-2 (free base) 【 分 子 式 】C9H15Cl2N5O2 【 分 子 量 】296.1582 |
【开发单位】Beiersdorf (Originator), Il-Yang (Licensee), Lilly (Licensee), Recordati (Licensee), Solvay (Licensee) 【药理作用】CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Imidazoline I1 Receptor Agonists |
合成路线1
The condensation of 5-amino 2 methyl 4,6-dichloropyrimidine (I) with 1-acetyl-2-imidazolin-2-one (II) by means of POCl3 at 50 C gives 4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-ylamino)pyrimidine (III), which is then methoxylated and desacetylated by treatment with sodium methoxide in refluxing methanol.
| 【1】 Mutsumi, M. (Nippon Chemiphar Co., Ltd.); Novel remedy for peptic ulcer. JP 1982075920 . |
| 【2】 Mannhold, R.; Moxonidine hydrochloride. Drugs Fut 1987, 12, 6, 553. |
| 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) | 23537 | 4,6-dichloro-2-methyl-5-pyrimidinamine; 4,6-dichloro-2-methyl-5-pyrimidinylamine | C5H5Cl2N3 | 详情 | 详情 | |
| (II) | 23538 | 1-acetyl-2-imidazolidinone | C5H8N2O2 | 详情 | 详情 | |
| (III) | 23539 | 1-[2-[(4,6-dichloro-2-methyl-5-pyrimidinyl)amino]-4,5-dihydro-1H-imidazol-1-yl]-1-ethanone | C10H11Cl2N5O | 详情 | 详情 |