论文部分内容阅读
α-三联噻吩(a-T)是一类具有优异性能的光活化农药.以三联噻吩为先导化合物,经a醛基化制得关键中间体2-醛基三联噻吩,然后与取代苯乙酮反应,得到三联噻吩取代的α,β-不饱和酮,再与盐酸羟胺、水合肼关环,最终合成两类含3,5-二芳基异噁唑和3,5-二芳基吡唑啉的α-三联噻吩衍生物.其结构经1H NMR,IR和元素分析确证.初步生物活性测定试验表明,绝大多数目标化合物具有良好的光活化活性,异噁唑类衍生物的光活化活性普遍要好于吡唑啉类衍生物,其中化合物3b光照前后的细胞毒杀活性差异为64.06倍.但部分吡唑啉类衍生物整体显示出较高的细胞毒杀活性,其中化合物4d光照细胞毒杀活性为83.9%.
α-tris-thiophene (aT) is a class of photo-activated pesticides with excellent properties. The key intermediates of 2-allyltristhiophene were prepared by a-allylation of thiophene with triphenylene, and then reacted with substituted acetophenones, To obtain trisubstituted thiophene α, β-unsaturated ketone, and then hydroxylamine hydrochloride, hydrazine hydrazine ring closure, the final synthesis of two types containing 3,5-diaryl isoxazole and 3,5-diaryl pyrazoline α-tris-thiophene derivatives.The structures were confirmed by 1H NMR, IR and elemental analysis.The preliminary bioassay showed that most of the target compounds had good photoactivation activity and the photoactivation activity of isoxazole derivatives was generally better Among the pyrazoline derivatives, the difference of the cytotoxic activity before and after irradiation of compound 3b was 64.06-fold, but some of the pyrazoline derivatives showed higher cytotoxic activity as a whole, in which the compound 4d phototoxic cytotoxic activity 83.9%.