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本文设计并合成了5-取代-4-甲基-1,3-二氢-2 H-咪唑-2-酮类化合物23个,其中19个尚未见报道。中间体5-(4-溴甲基苯甲酰基)-4-甲基-1,3-二氢-2H-咪唑-2-酮(Ⅴ)为一新化合物。在关键中间体4-甲基-1,3-二氢-2H-咪唑-2-酮(Ⅳ)的合成中,设计了由β-羟基丙胺一步氧化直接合成氨基丙酮的新方法。药理初筛表明:Ⅱ_1,Ⅱ_2,Ⅱ_4,Ⅲ_4,Ⅲ_6,Ⅲ_7,Ⅲ_8和RMI 82,249(1)具有不同程度的正性肌力作用,其中4个未知化合物Ⅱ_1,Ⅱ_2,Ⅱ_4和Ⅲ_4的最大效应高于已知对照物(1)。Ⅱ_4既增加心肌收缩力,又减慢心率,值得进一步研究。
In this paper, 23 5-substituted-4-methyl-1,3-dihydro-2H-imidazol-2-ones were designed and synthesized, of which 19 have not been reported yet. The intermediate 5- (4-bromomethylbenzoyl) -4-methyl-1,3-dihydro-2H-imidazol-2-one (V) is a new compound. In the synthesis of 4-methyl-1,3-dihydro-2H-imidazol-2-one (Ⅳ), a key intermediate, a novel method for the direct synthesis of aminoacetone from β-hydroxypropylamine by one-step oxidation was designed. Pharmacological preliminary screening showed that the inotropic effect of Ⅱ_1, Ⅱ_2, Ⅱ_4, Ⅲ_4, Ⅲ_6, Ⅲ_7, Ⅲ_8 and RMI 82,249 (1) had different degrees of inotropic effect. The maximal effect of four unknown compounds Ⅱ_1, Ⅱ_2, Ⅱ_4 and Ⅲ_4 In the known control (1). Ⅱ_4 not only increase myocardial contractility, but also reduce heart rate, it is worth further study.