摘要
目的研究抗真菌药物硫酸艾沙康唑中间体A的新工艺。方法以3-羟甲基-2-甲氨基吡啶为原料,经氯代、缩合步骤制备中间体A。结果成功制备了中间体A,总收率达54%。结论新工艺避开了不稳定中间体的同时,增强了各反应步骤的化学选择性,避免了缩合剂的使用,简化了操作步骤,具有反应条件温和、操作简便的优点,适用于工业化生产。
OBJECTIVE To study the newly process development of intermediate A towards syntheses of antifungal drug Isavuconazonium sulfate.METHODS 3-hydroxymethyl-2-methylamino-pyridine was employed to synthesize intermediate A via multi-step reactions including chlorination,condensation,and so on.RESULTS Intermediate A was obtained with 54%overall yield.CONCLUSION The new development synthetic process free of condensation reagents with mild reaction conditions and simple operation avoids the unstable intermediate and enhances the chemical selectivity of each step.It is suitable for the industrial production.
作者
李小丝
陆一菱
张善军
刘广宣
LI Xiaosi;LU Yiling;ZHANG Shanjun;LIU Guangxuan(Hospital of Chengdu Office of People's Government of Tibetan Autonomous Region,Chengdu,Sichuan,610000 P.R.China;The Third People's Hospital of Chengdu,Chengdu,Sichuan,610000 P.R.China;Chengdu Sino-Strong Pharmaceutical Co.,Ltd.,Chengdu,Sichuan,610000 P.R.China;Guizhou Province People's Hospital,Guiyang,Guizhou,550002 P.R.China)
出处
《华西药学杂志》
CAS
CSCD
2020年第3期240-243,共4页
West China Journal of Pharmaceutical Sciences
关键词
抗真菌药物
硫酸艾沙康唑
新工艺
化学选择性
中间体
工业化
3-羟甲基-2-甲氨基吡啶
Antifungal drug
Isavuconazonium sulfate
Newly process
Chemical selectivity
Intermediate
Industrial production
3-hydroxymethyl-2-methylamino-pyridine
