CAJ | 학술논문

以乙酰乙酸乙酯为原料,与原甲酸三乙酯、乙酸酐反应生成乙氧基衍生物,再与盐酸羟胺反应生成5-甲基-4-异噁唑甲酸甲酯,经水解、氯代后与对氟三甲基苯胺生成产物来氟米特,五步总收率29.2%。产品质量稳定,并成功的实现中试化生产。
이을선을산을지위원료,여원갑산삼을지、을산항반응생성을양기연생물,재여염산간알반응생성5-갑기-4-이오서갑산갑지,경수해、록대후여대불삼갑기분알생성산물래불미특,오보총수솔29.2%。산품질량은정,병성공적실현중시화생산。
Leflunomide was synthesized using ethyl acetoacetate as starting material,which reacted with triethyl orthoformate and acetic oxide to give ethoxymethylene derivative,and then cyclization,hydrolyzed and chloride to obtain the important intermediate.Finally,this compound was converted with 4-（trifluoromethyl） aniline into Leflunomide,The total ylied of five steps was 29.2%.The product had a stabile quality,and achieved industrial manufacturing successfully.