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6-甲基-2,4-二羟基嘧啶(6-MU)在无水乙醇中与甲醛和二乙胺反应,生成5-二乙氨甲基-6-甲基-2,4-二羟基嘧啶。实验研究了影响反应收率的各种因素,确定了优化的反应条件:6-MU∶二乙胺∶甲醛(摩尔比)=1∶2∶2,反应溶剂无水乙醇,溶剂量60 mL,反应时间3 h,产物收率34.9%。LS-MS和1H NMR对产品进行了结构鉴定,确定产品为5-二乙氨甲基-6-甲基-2,4-二羟基嘧啶。通过小鼠耳肿胀实验对该化合物进行抗炎活性的初步研究,结果表明低中高剂量组的5-二乙氨甲基-6-甲基-2,4-二羟基嘧啶与空白对照组比较均有显著差异,具有显著的抗炎作用。
6-Methyl-2,4-dihydroxypyrimidine (6-MU) is reacted with formaldehyde and diethylamine in absolute ethanol to give 5-diethylaminomethyl-6-methyl-2,4-dihydroxy Pyrimidine. The factors influencing the yield of the reaction were experimentally studied, and the optimal reaction conditions were determined: 6-MU: diethylamine: formaldehyde (molar ratio) = 1:2:2, The reaction time was 3 h and the product yield was 34.9%. LS-MS and 1H NMR of the product were identified, the product is identified as 5-diethylaminomethyl-6-methyl-2,4-dihydroxypyrimidine. The anti-inflammatory activity of the compound was evaluated by mouse ear swelling test. The results showed that 5-diethylaminomethyl-6-methyl-2,4-dihydroxypyrimidine was lower than the blank control group There are significant differences, with significant anti-inflammatory effect.