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本文报道了一系列2-氨基-3′-胺甲基-4′-羟基-6-取代异黄酮化合物(Ⅱ)的合成。中间体2-甲氧基-5-取代苯甲酸甲酯(Ⅲ)系用相转移催化技术同时进行醚化和酯化得到。Claisen缩合产物用三溴化硼脱甲基同时环化成2-氨基异黄酮化合物(Ⅵ)。利用Mannich反应在4′-羟基的邻位引入胺甲基制得目的物。药理筛选结果显示Ⅱbb′对小鼠具有明显的耐缺氧作用。
This paper reports the synthesis of a series of 2-amino-3’-aminomethyl-4’-hydroxy-6-substituted isoflavones (Ⅱ). The intermediate methyl 2-methoxy-5-substituted benzoate (Ⅲ) is obtained by the simultaneous phase etherification and esterification using phase transfer catalysis. The Claisen condensation product is deprominated with boron tribromide and simultaneously cyclized to the 2-aminoisoflavone compound (VI). The Mannich reaction was used to introduce the amine methyl group in the ortho position to the 4’-hydroxyl group to prepare the target compound. Pharmacological screening showed that Ⅱbb ’had obvious hypoxia tolerance in mice.