摘要
对氨基苯甲酸经重氮化后再与2-氯乙酰乙酸乙酯反应制得(Z)-4-[2-(1-氯-2-乙氧基-2-羰亚甲基)肼基]苯甲酸(1);1与二甲基环己二酮成环后再与对羟基环己胺完成酰胺化反应合成了一种新型Hsp90抑制剂——N-(4-羟基环己基)-4-[1-(6,6-二甲基-4-氧-3-乙酰氧基-4,5,6,7-四氢吲唑)]苯甲酰胺(3),其结构经1HNMR表征。荧光偏振法研究结果表明3对Hsp90α具有明显的抑制活性。
（Z） -4- [ 2- （ 1 -chloro-2-ethoxy-2-oxoethylidene ） hydrazinyl ] benzoic acid （ 1 ） was prepared from p-aminobenzoic acid by diazotization, then reacted with ethyl 2-chloro-acetoacetate. A novel Hsp90 inhibotor, ethyl 1 - { 4- [ （ 4-hydroxycyclohexyl ） carbamoyl ] phenyl } -6,6-dimethyl-4-oxo-4,5,6, 7-tetrahydro-lH-indazole-3-carboxylate（3）, was synthesized by cyclization between 1 and 5,5-dimethyl-cyclohexane-1,3-dione, then amidation with p-hydroxyl-cyclohexylamine. The structure was characterized by 1H NMR. The result from fluorescence polarization showed that 3 exhibited good inhibition against Hsp90α.
出处
《合成化学》
CAS
CSCD
北大核心
2011年第5期659-661,共3页
Chinese Journal of Synthetic Chemistry
