取代吡唑啉衍生物的合成与生物活性

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.

Studies on the Synthesis and Bioactivities of Substituted Dihydropyrazole Derivatives

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 ¹H 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.