Fufenozide 呋喃虫酰肼

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呋喃虫酰肼

CAS登记号:467427-81—1
英文名称:Fufenozide
化学名称:N一(2,3-_7-氢一2,7-二甲基.苯并呋喃.6一甲酰基)一N’一特丁基.N’.(3,5二甲基苯甲酰基)肼;
其他名称:JS118,福先
分子式:C24H30N2O3
分子量:394.5

Fufenozide

理化性质:白色粉末状固体;熔点:146.0—148.00C;溶-于有机溶剂,不溶于水。

毒性: 呋喃虫酰肼原药对大鼠急性经口LDso>5000mg/kg(雄,雌),大鼠急性经皮LDso>5000 mg/kg(雄,雌)均属微毒类农药。眼刺激试验为1.5(1h),对眼无刺激(1:100稀释)。皮肤刺激试验为0(4h),对皮肤无刺激性。Ames试验无致基因突变作用。

对10%呋喃虫酰肼悬浮剂进行了鱼、蜜蜂、鹌鹑、家蚕等4种环境生物的毒性试验,结果如下:斑马鱼IEso(96h)48rag/L;蜜蜂LCso(48h)>500rag/L;鹌鹑LDso(7d)>5000m#kg体重;家蚕LCso(2龄)0.7mg/kg桑叶。

根据农药对环境生物的急性毒性及风险评价分级标准,10%呋喃虫酰肼悬浮剂对鱼、蜜蜂、鸟均为低毒,对家蚕高毒;对蜜蜂低风险,对家蚕极高风险,桑园附近严禁使用。

作用特点及杀虫谱:福先为酰肼类化合物,是一类作用机理比较独特的杀虫剂,属于昆虫生长调节剂类。该药通过模拟昆虫蜕皮激素,甜菜夜蛾等幼虫取食福先后4~16h开始停止取食,随后开始蜕皮。24h后,中毒幼虫的头壳早熟开裂,蜕皮过程停止,幼虫头部与胸部之间具淡色间隔,引起早熟、不完全的蜕皮。出现的外部形态变化有,头壳裂开露出表皮没有鞣化和硬化的新头壳,经常形成“双头囊”,不表现出脱皮或脱皮失败,直肠突出,血淋巴和蜕皮液流失,末龄幼虫则形成幼虫-蛹的中间态等。中毒幼虫排出后肠,使血淋巴和蜕皮液流失,并导致幼虫脱水和死亡。福先主要具有胃毒作用,兼有触杀作用。另外,福先的作用位点和作用方式与有机磷类、菊酯类完全不同,故对抗性害虫也表现出高活性。

亩用10%呋喃虫酰肼悬浮剂6~8g可有效防治玉米田、蔬菜田发生的甜菜夜蛾。

产品特点
1、杀虫谱广,福先对甜菜夜蛾、斜蚊夜蛾、小菜蛾、茶尺蠖和各类螟虫等鳞翅目害虫有优异的防治效果。
2、高效,亩用有效成分5克,对大多数鳞翅目害虫达到控制作用。
3、毒性极低,对有益节肢动物和哺乳动物影响很小。
4、对抗性害虫效果好,其独特的作用机制使福先和其它杀虫剂没有交互抗性,对有机磷类、菊酯类等产生抗性的害虫的防治非常有效。因而福先在高毒品种替代和害虫综合治理中是一种理想的替换产品。
5、福先是一类作用机理比较独特的杀虫剂,属于昆虫生长调节剂类。
6、安全性好,福先对许多作物均表现出非常好的选择性。
7、作用方式以胃毒作用为主,同时具有一定的触杀作用。
8、实用性强,福先可与多种其它农药产品混用。

剂型:10%悬浮剂
生产方法: 以3-氯-2-甲基苯胺为起始原料,经过重氮化、醚化、重排、环合、氰化、水解、酰氯化、缩合等反应合成创制杀虫剂呋喃虫酰肼。合成总收率35.6%,原药含量97%.

生产情况:福先是江苏省农药研究所股份有限公司暨国家南方农药创制中心江苏基地自主创制发明的广谱高效、安全、实用、对环境友好的新型特异性杀虫剂,中国发明专利号:ZL 0118161.9。江苏省农药研究所股份有限公司建有500吨/年生产装置。

 

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Fufenozide

JS-118 is an extensively used insecticide in China. The present study investigated the genotoxic effect of JS-118 on whole blood at 24, 48, 72 and 96 h by using alkaline comet assay. Male Kunming mice were given 6.25, 12.5, 25, 50 and 100 mg/kg BW of JS-118 intraperitoneally. A statistically significant increase in all comet parameters indicating DNA damage was observed at 24 h post-treatment (p < 0.05). A clear concentration-dependent increase of DNA damage was revealed as evident by the OTM (arbitrary units), tail length (µm) and tail DNA (%). From 48 h post-treatment, a gradual decrease in mean comet parameters was noted. By 96 h of post-treatment, the mean comet tail length reached control levels indicating repair of damaged DNA. This study on mice showed different DNA damage depending on the concentration of JS-118 and the period of treatment. The present study provided further information of the potential risk of the genetic damage caused by JS-118.

Mode: insect growth regulator
Source: Organic Synthesis
Appearance: off-white powder
Development codes:JS118
Chemical Abstracts name: 6-benzofurancarboxylic acid, 2,3-dihydro-2,7-dimethyl-2-(3,5-dimethybenzoyl)-2-(1,1-dimethylethyl)-hydrazide
Biochemistry: Ecdysone agonist which acts by binding to the receptor site of the insect moulting hormone, ecdysone.
Mode of action:Lethally accelerates moulting process.

Formulation types: SC, WP
Fufenozide is a novel insecticide with Intellectual Property, safe to natural enemy of insect, for example, acarid, bees, pulse wing item, and beetle. Lower toxicity to mammalian such as people, domestic animal, aves, fish and bees. Fufenozide is provide with high efficiency to all lepidopterous pests which is dangerous to agricultural production at present and it also can be used on crops and forest to prevention lepidopterous pests, cotton, nut, apple, sugar cane, orange, rice, vegetable and sugar beet and so on. Proved by test, it is uneasy for pest to bring fastness after using Fufenozide ,especially on plutella xylostella. This character not only ensures the efficiency, but also solute the problem which efficiency decreases after pesticide fastness appears.

The mechanism of fufenozide is imitate ecdysone, which is an insect growth regulator with resemble living property.Attack insect growth and development system, restrain ecdysis and new cuticle form to prevention and cure pest.
Fufenozide can be used to prevention all kinds of lepidopterous pests in agricultural production, vegetable fruit, and economic crops, such as beet armyworm, Spodoptera litura, plutella xylostella, tea geometrid and all kinds of borers.Fufenozide is a high efficiency and lower poison green chemical pesticide and it only need 75g/ha.There is no similar product both in domestic and abroad.
Fufenozide is provide with high efficiency to all lepidopterous pests which is dangerous to agricultural production at present and it also can be used on crops and forest to prevention lepidopterous pests, cotton, nut, apple, sugar cane, orange, rice, vegetable and sugar beet and so on.

Insect Crop LC50/LD50
(mg/L , ug/pest)
Spodoptera exigua
Beet armyworm Vegetable, maize 3.055
Plutella xylostella
Diamond back moth Vegetable 69.04
Ectropis oblique
Tea geometrid Tea tree 26.01
Cnaphalocrocis medinalis
rice leaf roller rice
Chilo suppressalis
Rice striped borer rice 0.0216 ug/pest
Leucania separate
Oriental armyworm wheat < 3
Ostrinia furnacalis
Asiatic corn borer maize 48.69
Artogeia rapae
cabbage butterfly Vegetables 100% / 20ppm
Spodoptera exigua Savoy Cabbage 100% / 20ppm
Plutella xylostella Savoy Cabbage 100% / 20ppm
Heliothis armigera Soya 100% / 20ppm
Spodoptera frugiperda Savoy Cabbage 100% / 20ppm
Prodenia litura
tobacco caterpillar Vegetables, lawn 48.3% / 100ppm
Phyllocnistis citrella
citrus leaf-miner citrus 80% / 200ppm