5-(4-氯苯基)-N,N-二甲基-7-三氟甲基吡唑并[1,5-a]嘧啶-3-酰胺的合成和抗肿瘤活性测定  

Synthesis and antitumor activities research of 5-(4-chlorophenyl)-N,N-dimethyl-7-(trifluoromethyl) pyrazolo pyrimidine-3-carboxamide

作　　者：石磊[1] 刘凤芝[1] 张鑫[1] 

机构地区：[1]哈尔滨医科大学药学院,黑龙江哈尔滨150081

出　　处：《哈尔滨医科大学学报》2012年第6期556-558,共3页Journal of Harbin Medical University

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。Objective To synthesize 5- （4-chlorophenyl） -N, N-dimethyl-7- （ trifluoromethyl ） pyrazolo [ 1,5-a] pyrimidine-3-carboxamide, and to assay its antitumor activities. Methods Based on the general structm：e of pyrimidine processing antitumor activity, 5- （ 4-chlorophenyl ） -N, N-dimethyl-7- （ trifluoromethyl ） pyrazolo [ 1,5-a ] 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.

关 键 词：合成 抗肿瘤活性 5-氨基-1H-吡唑 

分 类 号：R979.1[医药卫生—药品]