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【结 构 式】 
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【药物名称】Nicorandil, RP-46417, SG-75, Adancor, Ikorel, Dancor, Sigmart 【化学名称】N-(beta-Hydroxyethyl)nicotinamide nitrate ester 【CA登记号】65141-46-0, 6265-73-2 (free base) 【 分 子 式 】C8H9N3O4 【 分 子 量 】211.17863 |
【开发单位】Chugai (Originator), Aventis Pharma (Licensee), Merck KGaA (Licensee) 【药理作用】Angina pectoris, Treatment of, CARDIOVASCULAR DRUGS, Cerebrovascular Diseases, Treatment of, Heart Failure Therapy, Hypertension, Treatment of, NEUROLOGIC DRUGS, Treatment of Disorders of the Coronary Arteries and Atherosclerosis, Vasodilators, K(ATP) Channel Activators |
合成路线1
The esteritication of nicotinic acid (I) with methanol and HCl or H2SO4 yields the corresponding methyl ester (II), which is treated with ethanolamine (A) to afford N-(beta-hydroxyethyl)nicotinamide (III). Finally, this compound is transformed into the nitrate ester by the usual methods.
| 【1】 Masayoshi, S.; Solubilizing agents. V. Pyridinecarboxamides. Yakugaku Zasshi 1960, 80, 1706-12. |
| 【2】 Thorpe, P.J.; Castaner, J.; SG-75. Drugs Fut 1979, 4, 2, 134. |
| 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) | 10259 | Ethanol amine;Ethanolamine;2-Aminoethanol; 2-Amino-1-ethanol；2-Aminoethyl alcohol | 141-43-5 | C2H7NO | 详情 | 详情 |
| (I) | 10752 | Nicotinic acid; Niacin | 59-67-6 | C6H5NO2 | 详情 | 详情 |
| (II) | 13980 | methyl nicotinate; Nicotinic acid, methyl ester | 93-60-7 | C7H7NO2 | 详情 | 详情 |
| (III) | 13982 | N-(2-Hydroxyethyl)nicotinamide | C8H10N2O2 | 详情 | 详情 |