卡奈替尼的合成工艺改进  

Improved synthesis of canertinib

作　　者：刘剑峰[1] 韩建奎[1] 侯桂华[2] 徐文方[3] 

机构地区：[1]山东大学齐鲁医院,山东济南250012 [2]山东大学医学院,山东济南250012 [3]山东大学药学院,山东济南250012

出　　处：《齐鲁药事》2011年第10期559-561,共3页qilu pharmaceutical affairs

摘　　要：目的改进抗肿瘤药物卡奈替尼的合成工艺。方法以2-氨基-4-氟苯甲酸和乙酸甲脒为起始原料,经环合、硝化、氯化、取代、氢化、酰化等反应制得抗肿瘤药物卡奈替尼。结果目标化合物的结构经1H-NMR谱和质谱确证。总收率为23.4%,比文献收率提高了17.2%。结论改进后的方法操作简便,有利于工业化生产。Objective To improve the synthetic procedure of canertinib. Methods Canertinib was synthesized from 2 - a- mino - 4 - fluorobenzoic acid and formamidine acetate via eyclization, nitration, ehlorinationb, substitution, hydrogenize, aeylation, etc. Results The structure of target compound was confirmed by 1 H - NMR, MS and the overall yield was 23.4%. Compared with the reported method, the overall yield was improved by 17.2%. Conclusion This synthetic process was suitable for industrial preparation.

关 键 词：2-氨基-4-氟苯甲酸 乙酸甲脒 卡奈替尼 抗肿瘤药 

分 类 号：TQ460.31[化学工程—制药化工]