【摘 要】
：
1,4-二氢吡啶是一类重要的含氮杂环化合物,大多具有生理活性,在药物合成与应用等领域得到广泛应用,其在临床上不仅用于治疗高血压、心绞痛、充血性心衰、局部缺血和动脉粥状硬化等心脑血管疾病,还用于治疗肠胃疾病、雷诺氏病以及作为治疗肺动脉高压和癫痫的辅药,因此国内外对该类化合物的研究十分活跃.Hantzsch反应是多组分合成1,4-二氢吡啶衍生物的经典和有效的方法.随着1,4-二氢吡啶衍生物多种生物活性
【机 构】
：
材料科学与化学工程学院,宁波大学,宁波315211
【出 处】
：
中国化学会第十三届全国有机合成化学学术研讨会
论文部分内容阅读
1,4-二氢吡啶是一类重要的含氮杂环化合物,大多具有生理活性,在药物合成与应用等领域得到广泛应用,其在临床上不仅用于治疗高血压、心绞痛、充血性心衰、局部缺血和动脉粥状硬化等心脑血管疾病,还用于治疗肠胃疾病、雷诺氏病以及作为治疗肺动脉高压和癫痫的辅药,因此国内外对该类化合物的研究十分活跃.Hantzsch反应是多组分合成1,4-二氢吡啶衍生物的经典和有效的方法.随着1,4-二氢吡啶衍生物多种生物活性的发现和该类药物的不断问世,Hantzsch反应已成为多组分反应研究的热点.Hantzsch反应为“一锅煮”串联反应一次形成多个化学键而生成新的化合物,具有操作简单、无需分离反应中间体、原子经济性高的特点,目前Hantzsch反应主要用于生物医药化合物、药物中间体的合成.因此,研究其合成的新方法对制药行业有重要的作用,对我国的制药业发展有重要意义.本文以对溴苯甲醛,对甲基苯甲醛,对、间、邻氰基苯甲醛,乙酰乙酸乙酯和醋酸铵为原料,采用超声微波法,通过“一锅煮”串联反应,设计合成了相应的1,4-二氢吡啶衍生物,考察了不同催化剂、取代基、溶剂等因素对Hantzsch反应收率的影响,并通过IR、NMR、UV-vis等光谱对合成化合物进行了分析表征.
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