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【结 构 式】 
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【药物名称】Piroximone, MDL-19205 【化学名称】4-Ethyl-1,3-dihydro-5-(4-pyridinylcarbonyl)-2H-imidazol-2-one 【CA登记号】84490-12-0 【 分 子 式 】C11H11N3O2 【 分 子 量 】217.22922 |
【开发单位】Aventis Pharma (Originator) 【药理作用】CARDIOVASCULAR DRUGS, Heart Failure Therapy, Phosphodiesterase III Inhibitors |
合成路线1
The acid chloride (II) of isonicotinic acid is prepared by reaction of oxalyl chloride (A) with the potassium salt of isonicotinic acid (I). The acylation of 1,3-dihydro-4-ethyl-2H-imidazol-2-one (III) with acid chloride (II) under Friedel-Crafts' conditions gives 1,3-dihydro-4-isonicotinoyl-5-ethyl-2H-imidazol-2-one.
| 【1】 Dage, R.C.; Schnettler, R.A.; Palopoli, F.P.; 4-Aroyl-1,3-dihydro-2H-imidazol-2-ones, a new class of cardiotonic agents. Effect of 4-Pyridoyl substituents and related compounds. 186th ACS Natl Meet (Aug. 28 - Sept. 2, Washington, D.C.) 1983, Abst MEDI-84. |
| 【2】 Schnettler, R.A.; Dage, R.C.; Grisar, J.M.; Palopoli, F.P.; 4-Pyridylimidazolones and method of use. EP 0059948; ES 8305352; ES 8402827; GB 2096600; US 4405628 . |
| 【3】 Mannhold, R.; Piroximone. Drugs Fut 1984, 9, 12, 905. |
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