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用十三种拟除虫菊酸合成了4-甲氧甲基苄基拟除虫菊酯及其α-氰基衍生物共十七种.为作比较,用类似的方法合成了3-苯氧基苄基拟除虫菊酯及其α-氰基衍生物共二十二种.对所有合成的酯用敏感系的蚊(幼虫及成虫),家蝇和(虫非)蠊作了生物活性测试.测试的结果显示: 4-甲氧甲基苄酯与著名的3-苯氧基苄酯对昆虫的生物活性互有上下,基本相当.前者的致死作用略低于后者,而对家蝇的击倒效果却优于后者.所以4-甲氧甲基苄醇可有效地作为合成拟除虫菊酯的醇组分. 3-苯氧基苄醇引上α-氰基后,其酯的致死作用得到增强,但其击倒作用变化却并不显著.而4-甲氧甲基苄醇引上α-氰基后,其酯的药效降低. 在所有新合成的拟除虫菊酯中,有三种4-甲氧甲基苄酯在所测定的生物活性方面优于生物烯丙菊酯,其中之一还具有良好的熏蒸效果,适用于蚊香,可代替天然除虫菊浸膏.
A total of 17 kinds of 4-methoxymethylbenzyl pyrethroids and their α-cyano derivatives were synthesized with thirteen pyrethoids. For comparison, 3-phenoxybenzyl A total of twenty-two pyrethroids and their α-cyano derivatives were tested for biological activity against all synthetic esters using susceptible mosquitoes (larvae and adults), houseflies and (pest) cockroaches. The results of the tests The results showed that the biological activity of 4-methoxymethylbenzyl ester and the famous 3-phenoxybenzyl ester on insects were similar to each other, the lethal effect of the former was slightly lower than the latter, but the knock-down effect on housefly But is superior to the latter, so 4-methoxymethylbenzyl alcohol can effectively act as the alcohol component of the synthetic pyrethroids.After 3-phenoxybenzyl alcohol is introduced into the α-cyano group, the lethal effect of the ester is enhanced , But its knockdown effect is not significant, while 4-methoxymethylbenzyl alcohol leads to the decrease of the pharmacophore of the ester after the addition of α-cyano group.Among all new synthetic pyrethroids, there are three 4- Methoxybenzyl is superior to bio-allethrin in its bioactivity assay, one of which also has a good fumigant effect and is suitable for mosquito coils and can replace natural pyrethrum extract.