1-(5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-1H-吡唑-3-基)-3-(吡啶-3-基甲基)脲的合成  

Synthesis of 1-(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazol-3-yl)-3-(pyridine-3-ylmethyl)urea

作　　者：陶晓璇[1] 郑志兵[1] 陈伟[1] 李松[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《化学试剂》2012年第7期581-584,共4页Chemical Reagents

基　　金：国家自然科学基金资助项目(81102308)

摘　　要：以5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-1H-吡唑-3-甲酸与二氯亚砜为起始原料,经酰氯化反应、酰胺反应、霍夫曼重排以及水解反应生成中间体5-(4-氯苯基)-1-(2,4-二氯苯基)-3-氨基-4-甲基-1H-吡唑,再经过与氯甲酸苯酯反应、胺酯交换反应得到标题化合物,其结构经1HNMR、MS谱确证,总收率26.9%。5-（4-chlorophenyl-1-（2,4-dichlorophenyl）-4-methyl-1H-pyrazol-3-carboxylic acid was acted as starting material,intermediate 5-（4-chlorophenyl-1-（2,4-dichlorophenyl）-4-methyl-1H-pyrazol-3-amino-4-methyl-1H-pyrazole was obtained via the reaction of acyl chloridation,amidation,Hoffman rearrangement and hydrolysis.Then the intermediate was reacted with phenyl chloroformate and at last the target compound was synthesized by the amine-ester exchange reaction.The structure was confirmed by MS and 1HNMR.The total yield was 26.9%.

关 键 词：CB1受体抑制剂 1-(5-(4-氯苯基)-1-(2 4-二氯苯基)-4-甲基-1H-吡唑-3-基)-3-(吡啶-3-基甲基)脲 Hofmann重排反应 

分 类 号：O622.6[理学—有机化学]