嘧苯胺磺隆水分散粒剂配方筛选研究

[目的]探讨嘧苯胺磺隆水分散粒剂的制备方法。[方法]研究采用湿法挤压制粒法制备嘧苯胺磺隆水分散粒剂的配方组成。[结果]嘧苯胺磺隆水分散粒剂的配方组成为:嘧苯胺磺隆原药60%,润湿剂为十二烷基硫酸钠K12(用量为2%),分散剂为亚甲基二萘磺酸钠NNO(用量为4%),崩解剂为羧甲基淀粉钠CMS-Na(用量为5%),填充剂为膨润土(补足100%),粘合剂为10%的淀粉浆。制备工艺为:将配方量的除粘合剂之外的其他组分用槽型混合机混合均匀,加入粘合剂制软材,用摇摆式颗粒机制粒,经干燥、筛分后得到最终产品。制得产品经热贮稳定性试验,各项质量指标均符合国家有关水分散粒剂的规定。[结论]试验结果为嘧苯胺磺隆的进一步推广应用提供了理论依据。

嘧苯胺磺隆水分散粒剂的田间药效及安全性研究

[目的]评价除草剂嘧苯胺磺隆水分散粒剂的田间药效及安全性。[方法]分别采用毒土法和喷雾法施药研究自行研制的60%嘧苯胺磺隆水分散粒剂对水稻的田间防效及安全性。[结果]该药剂对异形莎草、节节草及其他阔叶杂草均有良好的防除效果,推荐剂量为120~150 g/hm2（制剂剂量）,对水稻无明显药害现象,用药后15 d对水稻的株高、分蘖数均无影响,收获期考察出现增产。[结论]为该制剂的开发与推广提供了理论依据。

50%嘧苯胺磺隆水分散粒剂防除移栽稻田杂草效果及对后茬作物的影响

50%嘧苯胺磺隆水分散粒剂对水稻田禾本科杂草稗草、部分阔叶草及莎草均有较理想的防效,对移栽水稻安全,增产效果较明显。50%嘧苯胺磺隆水分散粒剂对水稻田后茬作物小麦、油菜、萝卜的安全性好。

嘧苯胺磺隆的合成与生物活性

[目的]嘧苯胺磺隆是嘧啶磺酰脲类除草剂,开展该类化合物的研究工作,探索其合成方法并进行生物活性测定。[方法]以邻氨基苯甲酸和2-氨基-4,6-二甲氧基嘧啶为起始原料,共经过4步反应合成目标化合物嘧苯胺磺隆,经核磁验证其结构。[结果]生物活性测定结果表明该化合物对苘麻具有优异的抑制效果。[结论]嘧苯胺磺隆具有优异的除草活性,且对水稻、小麦安全,具有很广阔的应用前景,值得重视。

Nichino America除草剂Craze^(TM)(嘧苯胺磺隆)在加州获登,用于葡萄、坚果类作物等

Nichino America公司除草剂CrazeTM现已在加利福尼亚获登,可用于葡萄、坚果类作物等。Craze含有活性成分嘧苯胺磺隆,被HRAC(除草剂抗性行动委员会)归入Group 2除草剂,它通过抑制植物乙酰乳酸合成酶(ALS)来阻断缬氨酸、亮氨酸和异亮氨酸等支链氨基酸的生物合成,从而导致植物死亡。Craze能够在苗前长效防控坚果和藤本植物中的杂草,包括四川锦葵、宝盖草(henbit)、藜、杉叶藻(marestail)等。Craze还能在苗前抑制难除的禾本科杂草和莎草香附子,对靶标杂草也具有苗后除草活性。田间试验表明,与其他ALS除草剂相比,Craze对阔叶杂草具与之有相同或更好的药效。

Residue and Degradation Dynamics of Bensulfuron-methyl·Mefenacet 4.2 g/kg Granule in Paddy Field

This study was conducted to determine the safety of bensulfuron-methyl and mefenacet in rice ecosystem. A field experiment was carried to reveal residual dynamics and final residue of bensulfuron-methyl.mefenacet 4.2 g/kg granule in rice and paddy system in Hangzhou, Changsha and Nanning of China during 2010 to 2011. The results showed that the average recoveries of bensulfuron-methyl and mefenacet spiked in the paddy soil, paddy water, rice, husk and rice plant at the 3 concentration levels of 0.05, 0.10 and 1.00 mg/kg ranged from 70.78% to 116.06% with the relative standard deviations of 0.91%-10.24%. The limit of detection （LOD） values of bensulfuron-methyl and mefenacet were 0.02 mg/L, and the minimum de- tection quantities were 4.0×10-9 g. The degradation dynamics test was done by spraying at a high dose （270 kg/hm2, bensulfuron-methyl active ingredient was 64.8 g/hm2, mefenacet active ingredient was 1 069.2 g/hm2） by direct spreading method 5-7 d after transplanting, and the final residual test carried out at a low dose （180 kg/hm2, bensuifuron-methyl active ingredient was 43.2 g/hm2, mefenacet active in- gredient was 712.8 g/hm2） and a high dose （270 kg/hm2）. The degradation research of bensulfuron-methyl and mefenacet in paddy water, soil and rice plant suggested that the degradation curves accorded with the first-order kinetics equation, the aver- age half life of bensulfuron-methyl was 5.35, 3.05 and 3.71 d in water, soil and rice plant, respectively, and the average half life of mefenacet was 3.61, 3.29 and 3.88 d in water, soil and rice plant, respectively. The final residues of bensulfuron-methyl and mefenacet were not detected in normal harvest paddy soil, rice straw, husk and brown rice.

新型磺酰脲类化合物的设计、合成与除草活性

[目的]利用中间体衍生化方法,设计合成一系列氨基磺酰脲类新化合物。[方法]以(取代)邻氨基苯甲酸为起始原料,通过与固体光气合环得到靛红酸酐,再与胺开环得到邻氨基苯甲酰胺中间体,最后再与嘧啶磺酰氯缩合得到磺酰脲类化合物。[结果]目标化合物结构经核磁表征。[结论]生物活性测定结果表明该类化合物具有较好的除草活性,可有效防除马唐和苘麻。并初步探讨了其结构活性关系。