合成五种喹唑啉类EGFR-TK抑制剂的新方法

A new approach to synthesizing five quinazolines as EGFR inhibitors

目的 :表皮生长因子受体酪氨酸激酶 (EGFR TK)是肿瘤治疗的一个新靶点 ,喹唑啉类化合物是一类有效的EGFR TK抑制剂 .其中 ,4 取代苯胺基 6 ,7 二甲氧基喹唑啉被证明有良好的抑制性 .我们改进了这种化合物的合成方法 ,用简单省时的SOCl2 回流法合成五种喹唑啉类EGFR TK抑制剂 .方法 :以 2 氨基 4 ,5 二甲氧基苯甲酸为原料 ,分别经过环化、氯代、取代等反应 ,合成了五种目标化合物 .结果 :经核磁光谱学数据鉴定 ,各中间体及目标产物均与其分子结构相符 .结论 :该合成方法简单、易行 ,操作简便 。

AIM: To synthesize 4 substituted aninine 6,7 dimethoxyl quinazoline, an effective epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. METHODS: A simple and timesaving SOCl 2 refluxed method was adopted to synthesize five quinazoline compounds as EGFR inhibitors. The five quinazoline compounds were prepared by using 2 amino 4,5 dimethoxy benzoic acid as original material, which underwent ring closing, halogenation and substitution. RESULTS: Intermediates and the five quinazolines were characterized by 1H NMR and were found to be in agreement with the corresponding molecular structures. CONCLUSION: This synthetic process is simple, convenient and cost saving.