1-甲基-3-三氟甲基-1H-吡唑-4-甲酸的合成  

Synthesis of 1-methyl-3-(trifluoromethyl)-1H-4-carboxylic acid

作　　者：李爱军[1,2] 吕恬恬 LI Ai-jun;LV Tian-tian(College of Chemical and Pharmaceutical Engineering,Hebei University of Science and Technology,Shijiazhuang 050018,China;State Key Laboratory Breeding Base-Kye Laboratory of Molecular Chemistry for Drug of Hebei Province,Shijiazhuang 050018,China)

机构地区：[1]河北科技大学化学与制药工程学院,河北石家庄050018 [2]河北省药用分子化学重点实验室,省部共建国家重点实验室培育基地,河北石家庄050018

出　　处：《化学研究与应用》2023年第4期997-1000,共4页Chemical Research and Application

摘　　要：通过Knoevenagel缩合反应、用甲基肼闭环、再用碱进行酯的水解,得到目标产物1-甲基-3-三氟甲基-4-吡唑甲酸。以三氟乙酰乙酸乙酯为原料,对比原甲酸三乙酯和N,N-二甲基甲酰胺二甲基缩醛与之反应所得中间体对后续反应的优劣。1-Methyl-3-(trifluoromethyl)-1H-pyrazole-4-carbonyl chloride was synthesized from ethyl 4,4,4-trifluoroacetoacetate via three steps including Knoevenagel condensation reaction,cyclization,hydrolysis.Using ethyl trifluoroacetate as raw material,the advantages and disadvantages of the intermediate obtained from the reaction of triethyl orthoformate and N,N-dimethyl-formamide dimethyl acetal on the subsequnt reaction was compared.

关 键 词：有机合成 工艺优化 闭环反应 克脑文盖尔缩合反应 

分 类 号：O626.21[理学—有机化学]