含联苯基的吡唑衍生物的合成及生物活性测试  

Synthesis and biological activity assay of pyrazol derivatives with biphenyl

作　　者：陈勇[1] 武文昌 夏雨 魏文博 CHEN Yong;WU Wenchang;XIA Yu;WEI Wenbo(Chemistry＆Chemical Industry School,Anyang Normal University,Anyang 455000,China)

机构地区：[1]安阳师范学院化学化工学院,河南安阳455000

出　　处：《化学研究与应用》2018年第6期978-984,共7页Chemical Research and Application

基　　金：河南省高等学校重点科研项目(192109316007)资助;河南省光电功能材料重点实验室项目资助

摘　　要：以2,4-二氟代联苯为原料,经傅-克酰基化、缩合、环化等反应步骤,合成了新型含联苯基的吡唑衍生物(4a^4k),其结构用红外光谱(IR)、高分辨质谱(HRMS-ESI)、核磁共振氢谱(~1H NMR)、核磁共振碳谱(13C NMR)进行了表征。测试了目标化合物(4a^4k)对Aurora激酶A的抑制活性,初步的测试结果表明,化合物4f对Aurora激酶A有一定程度的抑制活性。The novel pyrazol derivatives（ 4 a - 4 k） with biphenyl were synthesized via F-C acylation,condensation,cyclization reaction starting from 2,4-difluorin-bipheny.The structure of the target compounds（ 4 a - 4 k） were confirmed by IR,-1H NMR,-（13）C NMR and HRMS-ESI spectra. The inhibition activity for Aurora kinase A of the target compounds were tested,preliminary test results showed that the compound 4 f had a certain degree of inhibitory activity for Aurora kinase A.

关 键 词：2 4-二氟联苯 吡啶 呋喃 吡唑衍生物 生物活性 

分 类 号：O626[理学—有机化学]