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为了寻求新颖的螺环季酮酸先导化合物,以3-(2,4-二氯苯基)-4-羟基-1-氧杂螺[4.5]癸-3-烯-2-酮为原料,合成了21个螺环季酮酸衍生物,其结构经1H NMR,ESI MS和元素分析确认,并测定了化合物6b的晶体结构.初步生物活性测定表明,此类化合物对朱砂叶螨、蚜虫和粘虫都具有很好的生物活性,尤其是化合物5g和5m对朱砂叶螨的LD50分别为35.12和22.39 mg/L,高于螺螨酯的LD50:45.20 mg/L;化合物5b对蚕豆蚜的LD50为21.90 mg/L,而螺螨酯对蚕豆蚜的LD50为174.13 mg/L.
In order to find a novel spirocyclic keto lead compound, 3- (2,4-dichlorophenyl) -4- hydroxy-1-oxaspiro [4.5] dec-3- 21 spirocyclic keto acid derivatives were synthesized and their structures were confirmed by 1H NMR, ESI MS and elemental analysis, and the crystal structure of compound 6b was also determined.The preliminary bioassay showed that the compounds were effective against spider mites, aphids and The armyworms had good biological activity, especially LD50 of compound 5g and 5m for Tetranychus cinnabarinus were 35.12 and 22.39 mg / L, respectively, which were higher than that of spirodiclofen. LD50: 45.20 mg / L; LD50 was 21.90 mg / L, while spirodiclofen had a LD50 of 174.13 mg / L for A. faba.