盐酸阿莫罗芬合成研究与进展  

Research and Progress Synthesis of the Amorlfine

作　　者：邓宁 施志豪 梁明明 梁萧斌 苏为科[1] 刘峰帆 DENG Ning;SHI Zhihao;LIANG Mingming;LIANG Xiaobing;SU Weike;LIU Fengfan(Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals,Zhejiang University of Technology,Hangzhou 310014)

机构地区：[1]浙江工业大学长三角绿色制药协同创新中心,杭州310014

出　　处：《化工生产与技术》2022年第2期27-33,I0004,共8页Chemical Production and Technology

摘　　要：归纳了目前报道的11种阿莫罗芬的合成方法,分别以叔戊基苯、对叔戊基苯甲醛、α-甲基肉桂酸、α-甲基肉桂醛和3-(4-叔戊基苯基)-2-甲基丙醇为起始原料,根据不同的起始原料合成阿莫罗芬,并且探讨了这些合成方法的优缺点。基于现有研究,以叔戊基苯、α-甲基肉桂酸和3-(4-叔戊基苯基)-2-甲基丙醇为起始原料总收率高、成本低,是工业化生产考虑的工艺路线。认为形成多步骤串联反应,减少后处理操作,寻找1条合成便宜起始原料的方法和替代Lewis酸催化体系是优化工艺路线的关键。Eleven reported methods for the synthesis of amorrofen were summarized.Amorrofen was synthesized from tertamylbenzene,p-tert-amylbenzaldehyde,α-methylcinnamic acid,α-methylcinnamic aldehyde and 3-(4-tert-amylphenyl)-2-methylpropanol with different starting materials,and the advantages and disadvantages of these methods were discussed.Based on the existing studies,using tert-amyl benzene,α-methyl cinnamic acid,and 3-(4-tert-amyl phenyl)-2-methylpropanol as starting materials have high overall yield and low cost,which is a process route for industrial production.It is believed that the key to optimizing the process route is to form a multi-step series reaction,reduce the post-processing operation,find a method for synthesizing cheap starting materials and replace the Lewis acid catalytic system.

关 键 词：阿莫罗芬 合成方法 抗真菌药 

分 类 号：TQ463[化学工程—制药化工]