论文部分内容阅读
基于萘普生的构效关系对其羧基进行结构修饰,设计合成了萘普生2-芳基吗啉乙酯类化合物.芳基乙酮经过溴代、胺化、还原得到的2-芳基-4-羟乙基吗啉在三乙胺作缚酸剂存在下与萘普生酰氯反应得到萘普生2-芳基吗啉乙酯类化合物,收率24.2%～76.5%.新化合物结构经1H NMR确认.生物活性实验结果表明:在10μmol/L质量浓度时,化合物1d对COX-2的抑制率达96.32%.
Based on the structure-activity relationship of naproxen, structural modification of its carboxyl group, the design and synthesis of naproxen 2-aryl morpholine ethyl ester compounds.Aryl ketone through bromination, amination, reduction of 2-aryl -4-hydroxyethyl morpholine reacted with naproxen in the presence of triethylamine as acid-binding agent to give naproxen 2-arylmorpholine ethyl ester, yield 24.2% -76.5% .New compound structure The results of 1H NMR showed that the inhibitory rate of compound 1d to COX-2 was 96.32% at the concentration of 10μmol / L.