取代吡唑啉衍生物的合成与生物活性  

Studies on the Synthesis and Bioactivities of Substituted Dihydropyrazole Derivatives

作　　者：刘天麟[1] 余盛良[1] 喻爱明[1] 

机构地区：[1]南开大学元素有机化学研究所

出　　处：《高等学校化学学报》1998年第2期232-236,共5页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金;南开大学科学基金

摘　　要：采用α－三唑－β－烷氧基芳酮与肼关环，制备了１，３－二苯基－４－三唑基吡唑啉１ａ，１－苯基－３－对氯苯基－４－三唑基吡唑啉１ｂ和３－取代苯基－４－三唑基吡唑啉（７），并研究了化合物７的成环优化条件．使用α，β－不饱和酮与肼关环合成了１，３，４，５－多取代吡唑啉衍生物１ｃ—１ｈ，并初步用质谱法确定了该反应产物的结构；同时，以３，５－二取代吡唑啉（６）和７作为中间体合成了１－，３－，４－或５－取代的化合物２ａ—２ｌ．初步生物活性测定结果表明，所合成的化合物均有一定的杀菌、激素和除草效果．A novel and convenient synthetic method for 1 phenyl 3 substituted phenyl 4 triazolyldihy dropyrazoles(1a 1b) and 3 substituted phenyl 4 triazolyldihydropyrazole (7) from α triazolyl β alkoxyacetophenone 4 was described. The reaction condition was studied and optimized. 1,3,4,5 Multi substituted dihydropyrazole 1c 1h were prepared through the general cyclization of α , β unsaturated ketone with phenylhydrazine and their structures were confirmed by 1 H NMR, MS and elemental analysis. Furthermore, 3,5 substituted dihydropyrazole 6(or 7) reacted with methyl(or ethyl) chloroformate and potassium thiocyanate to afford 1,3,5 (or 4 )substituted dihydropyrazole 2a 2l. The results of preliminary bioassay presented that almost all compounds showed fungicidal, herbicidal and plant growth regulatory activities.

关 键 词：合成 生物活性 吡唑啉衍生物 取代基 

分 类 号：O626.21[理学—有机化学]