摘要
2-氯-4,6-二甲氧基-1,3,5-三嗪和N-甲基吗啉反应得到氯化4-(4,6-二甲氧基-1,3,5-三嗪-2-基)-4-甲基吗啉,其与5-甲基异唑-4-甲酸反应制备2-(5-甲基异唑-4-甲酰氧基)-4,6-二甲氧基-1,3,5-三嗪,所得化合物与4-三氟甲基苯胺反应合成标题化合物,总收率约72%(以5-甲基异唑-4-甲酸计)。
2-Chloro-4,6-dimethoxy-1,3,5,-triazine was reacted with N-methylmorpholine to give 4-（4,6-dimethoxy-1,3,5-triazin-2-yl）-4-methylmorpholinium chloride.4-（4,6-dimethoxy-1,3,5-triazin-2-yl）-4-methylmorpholinium chloride was reacted with 5-methylisoxazole-4-carboxylic acid to obtain2-（5-methylisoxazole-4-methanoyl）-4,6-dimethoxy-1,3,5,-triazine.2-（5-methylisoxazole-4-methanoyl）-4,6-dimethoxy-1,3,5,-triazine was coupled with 4-trifluoro-methyl aniline to give Leflunomide with an overall yield of about 72%（based on 5-methylisoxazole-4-carboxylic acid）.
出处
《化学试剂》
CAS
CSCD
北大核心
2011年第10期948-950,共3页
Chemical Reagents
关键词
来氟米特
类风湿关节炎
合成
活性酯
leflunomide
rheumatoid arthritis
synthesis
active ester
