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乙酰胆碱酯酶抑制剂4-芳胺基喹唑啉的绿色合成

Green synthesis of 4-arylaminoquinazoline of acetylcholinesterase inhibitors
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摘要 4-芳胺基喹唑啉是十分有效的表皮生长因子受体(EGFR)抑制剂,是抗癌药物研制的热点之一.本研究以邻氨基苯腈、DMF-DMA、苯胺为原料,探索多相催化过程,并通过溶剂、反应温度等工艺条件的优化提高目标产物4-芳胺基喹唑啉合成工艺的绿色化程度.研究表明,非均相催化剂磺化硅胶对喹唑啉的合成具有易于实施、过程简单、选择性好及环境友好等特点,大大提高了制备工艺的原子经济性和绿色化水平. 4-Arylaminoquinazoline has become one of hot research spots as anticancer pharmaceuticals for its effective inhibition of epidermal growth factor receptor（EGFR）. In order to increase the green degree of the synthesis process of 4-arylaminoquinazolines,heterogeneous catalytic reaction was investigated using 2-aminobenzonitrile and DMF-DMA as reactants in this study,and its solvent types and reaction temperature were optimized. The study shows that for the synthesis of 4-arylaminoquinazolines,the heterogeneous catalyst sulfonated silica gel is easy to implement,simple in process,good at selectivity and environmentally benign,thus greatly increase the atom economy and green level of preparation technology.
作者 陈宝龙 张翔 李恒 游震生 冯甜 张立军
机构地区 天津理工大学化学化工学院
出处 《天津理工大学学报》 2016年第3期55-59,共5页 Journal of Tianjin University of Technology
基金 国家自然科学基金(21176193)
关键词 喹唑啉 乙酰胆碱酯酶抑制剂 绿色合成 quinazoline acetylcholinesteras inhibitor green synthesis
分类号 O621.3 [理学—有机化学]
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参考文献18

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天津理工大学学报
2016年 第3期

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