中国生化药物杂志
中國生化藥物雜誌
중국생화약물잡지
Chinese Journal of Biochemical Pharmaceutics
2015年
9期
4-7
,共4页
宋盼盼%张首国%彭涛%温晓雪%明琰%王林
宋盼盼%張首國%彭濤%溫曉雪%明琰%王林
송반반%장수국%팽도%온효설%명염%왕림
c-Met%合成%类似物%抗肿瘤
c-Met%閤成%類似物%抗腫瘤
c-Met%합성%유사물%항종류
c-Met%synthesis%analogue%antitumor
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1 H-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。
目的：閤成小分子c-Met激酶抑製劑類似物N-（4-氟苯基）-N-（4-苯氧基苯基）環丙烷-1，1-二甲酰胺（ NFNPDB）。方法以丙二痠二乙酯為起始原料經親覈取代、酰胺化、芳香醚化、還原和縮閤等反應閤成NFNPDB。結果目標產物總產率為3.79％，其結構經1 H-NMR確證。結論本文研究的NFNPDB閤成方法成本低、路線短、操作簡便，為進一步設計閤成新的小分子c-Met激酶抑製劑奠定瞭基礎。
목적：합성소분자c-Met격매억제제유사물N-（4-불분기）-N-（4-분양기분기）배병완-1，1-이갑선알（ NFNPDB）。방법이병이산이을지위기시원료경친핵취대、선알화、방향미화、환원화축합등반응합성NFNPDB。결과목표산물총산솔위3.79％，기결구경1 H-NMR학증。결론본문연구적NFNPDB합성방법성본저、로선단、조작간편，위진일보설계합성신적소분자c-Met격매억제제전정료기출。
Objective To synthesize N-(4-fluorophenyl)-N-(4-phenoxyphenyl) cyclopropane-1,1-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.
