N-(4-氟苯基)-N-(4-苯氧基苯基)环丙烷-1,1-二甲酰胺的合成研究  

Synthesis of N-( 4-fluorophenyl)-N-( 4-phenoxyphenyl)cyclopropane-1,1-dicarboxamide

作　　者：宋盼盼[1,2] 张首国[2] 彭涛[2] 温晓雪[2] 明琰[3] 王林[2] 

机构地区：[1]安徽医科大学 [2]军事医学科学院放射与辐射医学研究所 [3]中国人民解放军62301部队

出　　处：《中国生化药物杂志》2015年第9期4-7,共4页Chinese Journal of Biochemical Pharmaceutics

基　　金：国家自然科学基金(81072531;81273431;21102176)

摘　　要：目的合成小分子c-Met激酶抑制剂类似物N-(4-氟苯基)-N-(4-苯氧基苯基)环丙烷-1,1-二甲酰胺(NFNPDB)。方法以丙二酸二乙酯为起始原料经亲核取代、酰胺化、芳香醚化、还原和缩合等反应合成NFNPDB。结果目标产物总产率为3.79%,其结构经1H-NMR确证。结论本文研究的NFNPDB合成方法成本低、路线短、操作简便,为进一步设计合成新的小分子c-Met激酶抑制剂奠定了基础。Objective To synthesize N-（4-fluorophenyl）-N-（4-phenoxyphenyl） cyclopropane-I ,1-dicarboxamide （NFNPDB） as small molecular c-Met kinase inhibitor analogue. Methods N-（ 4-fluorophenyl ）-N-（ 4-phenoxyphenyl ） cyclopropane-1, 1-dicarboxamide was synthesized by nucleophilicsubstitution, amidation, etherification, reduction and condensation from diethyl malonate. Results The total yield of target compound was 3.79% , its structure was confirmed by 1 H-NMR. Conclusion The synthesis method of NFNPDB in our research can be easily operated with lost cost and short direction, which lays the foundation for designing the synthetic process of newly small molecular c-Met kinase inhibitor.

关 键 词：C-MET 合成 类似物 抗肿瘤 

分 类 号：R625[医药卫生—整形外科]