卡奈替尼的合成工艺改进

Improved synthesis of canertinib

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.