【摘要】 目的合成5-(4-氯苯基)-N,N-二甲基-7-三氟甲基吡唑并[1,5-a]嘧啶-3-酰胺,并评价其抗肿瘤活性。方法根据吡唑并[1,5-a]嘧啶类抗肿瘤药物的基本结构,设计了5-(4-氯苯基)-N,N-二甲基-7-三氟甲基吡唑并[1,5-a]嘧啶-3-酰胺,并以乙氧基甲叉基氰乙酸乙酯和对氯苯乙酮为起始原料,经4步反应得到目标产物。以环磷酰胺为阳性对照药,通过体内试验,对目标化合物进行抗肿瘤活性测定。结果合成了3个未见文献报道的新化合物,结构经IR和1 H-NMR确证。结论化合物7显示出较好的抗肿瘤活性。更多还原

【Abstract】 Objective To synthesize 5-(4-chlorophenyl)-N,N-dimethyl-7-(trifluoromethyl) pyrazolo pyrimidine-3-carboxamide,and to assay its antitumor activities.Methods Based on the general structure of pyrazolo pyrimidine processing antitumor activity,5-(4-chlorophenyl)-N,N-dimethyl-7-(trifluoromethyl) pyrazolo pyrimidine-3-carboxamide was designed,and the target compound was synthesized via a 4-step procedure starting from Ethyl(ethoxymethylene) cyanoacetate and 4-Chloroacetophenone.With CTX as a positive control,the target compound for anti-tumor activity was measured in vivo.Results Three novel compounds were synthesized,and their structures were confirmed by IR and 1 H-NMR.Conclusion Compound 7 displays good antitumor activities.更多还原