摘要
以 N,N-二甲基甲酰胺缩醛与乙酰乙酸乙酯缩合后无需分离 ,经环合、水解得到 5 -甲基异唑 - 4-甲酸 ,收率5 6 %,再经酰氯化、与对三氟甲基苯胺反应得到来氟米特。总收率 47.8%(按乙酰乙酸乙酯计 )
A facile method was developed for the synthesis of leflunomide. N ,N - Dimethylfor- mamide reacted with dimethyl sulfate to give N,N - dimethylformamide dimethyl acetal,and then con- densed with ethyl acetoacetate to obtain intermediate4,which underwent cyclization and hydrolysis to afford 5 - methylisoxazole- 4- carboxylic acid (6 ) . The acyl chloride of 6 reacted with p- trifluo- romethylaniline to obtain leflunomide in an overall yield of47.8%(from ethyl acetoacetate) .
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2002年第2期53-55,共3页
Chinese Journal of Pharmaceuticals
