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【结 构 式】

【药物名称】Fenoximone, Enoximone, MDL-17043, RMI-17043, Perfan, Perfane

【化学名称】4-Methyl-5-[p-(methylthio)benzoyl]-4-imidazolin-2-one
      1,3-Dihydro-4-methyl-5-[4-(methylthio)benzoyl]-2H-imidazol-2-one

【CA登记号】77671-31-9

【 分 子 式 】C12H12N2O2S

【 分 子 量 】248.30564

【开发单位】Aventis Pharma (Originator), Lepetit (Originator), Myogen (Licensee)

【药理作用】CARDIOVASCULAR DRUGS, Heart Failure Therapy, cAMP Phosphodiesterase Inhibitors, Phosphodiesterase III Inhibitors

合成路线1

The reaction of 4-(methylthio)benzoic acid (I) with SOCl2 in refluxing benzene gives 4-(methylthio)benzoyl chloride (II), which is then condensed with 1,3-dihydro-4-methyl-2H-imidazol-2-one (III) by means of AlCl3 in hot nitrobenzene.

1 Dage, R.C.; Schnettler, R.A.; Grisar, J.M. (Aventis Pharmaceuticals, Inc.); 4-Aroylimidazol-2-ones. BE 0883856; DE 3021792; FR 2459233; GB 2055364; JP 56005463 .
2 Pento, J.T.; Serradell, M.N.; Castaner, J.; Blancafort, P.; RMI-17,043. Drugs Fut 1983, 8, 4, 343.
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) 30683 4-(methylsulfanyl)benzoic acid 13205-48-6 C8H8O2S 详情 详情
(II) 21238 4-(methylsulfanyl)benzoyl chloride C8H7ClOS 详情 详情
(III) 30684 4-methyl-1,3-dihydro-2H-imidazol-2-one C4H6N2O 详情 详情
Extended Information