2-氨基查尔酮类化合物的简便合成

Facile Synthesis of 2-Aminochalcones

2-氨基查尔酮类化合物是一类重要的合成中间体,在药物化学、有机合成等领域有广阔的应用前景。现有合成方法大多存在原料不易得、底物范围窄、收率较低等问题。发展了一种利用查尔酮和叠氮钠制备目标化合物的方法。该反应无需催化剂,在CO_(2)氛围中,120℃反应5 h以较高收率获得目标化合物。该合成方法体系简单,具有原料价廉易得、后处理操作简便、底物范围广等优点。

2-Aminochalcones are a class of important intermediates and have broad application prospects in the fields of medicinal chemistry and organic synthesis.Most of the existing synthetic methods have problems,such as difficult synthesis of raw materials,narrow substrate range,and low yield.A method for preparing the title compounds using chalcones and sodium azide has been developed.The method does not require a catalyst,and reacts at 120℃for 5 h in CO_(2) atmosphere to obtain the title compounds in high yields.The synthetic method has the advantages of low cost,readily availability of raw materials,simple operation and workup,and wide substrate range.