尼达尼布的合成工艺改进  

Research on improvement on the synthesis process of nintedanib

作　　者：杨怡[1] 刘巧云[1] 赵金亮 王菲 Yang Yi;Liu Qiaoyun;Zhao Jinliang;Wang Fei(Changzhou Vocational Institute of Engineering,Changzhou 213164,China;Changzhou Jiade Pharaceutical Technology Co.,Ltd.,Changzhou 213164,China)

机构地区：[1]常州工程职业技术学院,江苏常州213164 [2]常州佳德医药科技有限公司,江苏常州213164

出　　处：《江苏科技信息》2019年第26期63-66,共4页Jiangsu Science and Technology Information

基　　金：2017年江苏省大学生创新创业训练计划项目;项目名称:特发性肺纤维化Ⅲ类新药尼达尼布关键中间体的研发

摘　　要：文章以2-氧化吲哚-6-甲酸甲酯、原苯甲酸三乙酯和醋酐为起始原料反应得到关键中间体:(E)-1-乙酰基-3-(乙氧基-苯基-甲烯基)-2-氧-2,3-二氢-1H-吲哚-6-甲酸甲酯(4),再与另一起始原料N-(4-氨基苯基)-N-甲基-2-(4-甲基哌嗪-1-基)乙酰胺(3)缩合得尼达尼布,纯度99.8%,总收率62.7%。In this paper,the key intermediate is prepared by the reaction of 2-oxidation of methyl-6-methyl formate,triethyl benzoate and vinegar as the starting material.(E)-1-acetylgroup-3-(ethoxy-phenyl-methenyl)-2-oxo-2,3-dihydro-1H-indole-6-methyl formate methyl ester(4),and then condensed with another starting material,N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide(3),forming nintedanid.The purity is 99.8%and the total yield is 62.7%.

关 键 词：尼达尼布 特发性肺纤维化 合成 

分 类 号：O6[理学—化学]