新型香豆素类药物中间体的合成

Synthesis of New Coumarin Derivatives

以2,3,4-三甲氧基苯甲醛(1)为原料,通过甲氧基还原反应、Knoevenagel反应缩合关环,再经硝基还原得到关键中间体3-氨基-7,8-二甲氧基香豆素,并以其为母体,将3位氨基酰化,获得3个新的3位酰氨基取代的7,8-二甲氧基香豆素,其结构经1 H NMR、13 C NMR、IR分析确证。考查了各种反应条件对中间体(2)产率的影响,确定最佳工艺条件为:n1∶nAlCl3=1∶1、甲苯90mL、反应温度80±2℃,反应时间4h。

With 2,3,4-trimethoxybenzaldehyde（1）as raw material,through the methoxy reduction reaction,Knoevenagel condensation reaction,amino reduction reaction and acetylation reaction three new 3-amide-substituted 7,8-dimethoxy coumarin derivatives were synthesized.Their structure was confirmed by 1 H NMR,13C NMR and IR analysis.The effect of reaction conditions on the yield of reaction intermediate（2）was studied.The optimum conditions were found as follows：n1∶nAlCl3=1∶1,toluene 90mL, reaction temperature 80±2℃and reaction time 4h.