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以诺蒎酮为原料,合成了新型蒎烷基吡唑酰胺类衍生物,并对其生物活性进行了研究.诺蒎酮与芳香醛进行缩合反应,得到中间体3-芳亚甲基诺蒎酮2a~2g,2a~2g与水合肼经环化、脱氢芳构化反应,得到新型蒎烷基吡唑类化合物3a~3g;以N,N-二甲基甲酰胺为溶剂,3a~3g与2-氯乙酰胺在碱催化作用下,合成了7种吡唑酰胺类化合物4a~4g.其结构经~1H NMR,~(13)C NMR,IR,和HRMS表征.通过X射线衍射分析测定了化合物2-(6’,6’-二甲基-3’-(4’-甲氧基苯基)-4’,5’,6’,7’-四氢-5’,7’-桥亚甲基-吲唑-1’-基)乙酰胺(4d)的晶体结构.探讨了化合物3a~3g和4a~4g的抑菌活性和对蚜虫的杀虫活性.实验结果表明,2-(6’,6’-二甲基-3’-(4’-氟苯基)-4’,5’,6’,7’-四氢-5’,7’-桥亚甲基-吲唑-1’-基)乙酰胺(4g)既具有较好的抑菌效果,同时对紫薇蚜虫也表现出较好的杀虫活性.
The new pinapyrazole derivatives were synthesized from nopronone and their biological activities were studied.Noconpineone was condensed with aromatic aldehyde to obtain the intermediate 3-arylmethylenenappin Ketone 2a ~ 2g, 2a ~ 2g and hydrazine hydrate by cyclization, dehydroaromatization reaction, to obtain novel pinanyl pyrazoles 3a ~ 3g; N-, N- dimethylformamide as solvent, 3a ~ 3 g and 2-chloroacetamide were synthesized under the catalysis of base, and 7 kinds of pyrazole amides were synthesized, whose structures were characterized by 1H NMR, 13 C NMR, IR and HRMS, respectively. The structures of the compounds were characterized by X-ray diffraction The compounds 2- (6 ’, 6’-dimethyl-3’- (4’- methoxyphenyl) -4’, 5 ’, 6’, 7’- tetrahydro- 5 ’, 7 ’- bridged methylene-indazol-1’-yl) acetamide (4d). The antibacterial activities and the insecticidal activities against aphids of the compounds 3a ~ 3g and 4a ~ 4g were discussed. Methyl 2- (6 ’, 6’-dimethyl-3’ - (4’-fluorophenyl) -4 ’, 5’, 6 ’, 7’-tetrahydro- -indazol-1’-yl) acetamide (4 g) has good antibacterial activity and also shows good insecticidal activity against crape myrtle aphids.