合成五种喹唑啉类EGFR-TK抑制剂的新方法

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，降低了反应成本．

A new approach to synthesizing five quinazolines as EGFR inhibitors

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.