No evidence of decomposition with presence of iron, aluminum or tin powder over 30-150 °C, degrades at 40-90 °C in the presence of /iron chloride/ powder. /from table/
Metabolism of isoxaflutole in ruminants proceeded via hydrolysis of the isoxazole ring to form RPA 202248 and RPA 205834 (further hydrolysed to produce RPA 207048).
In a metabolism study /in rats/, ...RPA 202248, a major metabolite, a diketonitrile derivative, represented 70% or more of the radioactivity excreted in the urine and feces from the two lowest dose groups. The other minor metabolite, RPA 203328, was more polar.
Metabolism of isoxaflutole in poultry involved hydrolysis of the isoxazole ring to form RPA 202248 and RPA 205834. Metabolite RPA 205834 was further hydrolysed to produce RPA 207048 (further degrades to RPA 203328) and RPA 203328. Hens were dosed (gelatin capsule) at a dietary burden of 10 ppm for 14 consecutive days.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类：可能对人类致癌
Cancer Classification: Likely to be Carcinogenic to Humans
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌物分类
未列在IARC（国际癌症研究机构）的名单上。
Not listed by IARC.
来源:Toxin and Toxin Target Database (T3DB)
毒理性
副作用
职业性肝毒素 - 第二性肝毒素：在职业环境中的毒性效应潜力是基于人类摄入或动物实验的中毒案例。
Occupational hepatotoxin - Secondary hepatotoxins: the potential for toxic effect in the occupational setting is based on cases of poisoning by human ingestion or animal experimentation.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
毒性数据
大鼠LC50 = 5,230毫克/立方米/4小时
LC50 (rat) = 5,230 mg/m3/4h
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
/SRP:/ Basic treatment: Establish a patent airway. Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with normal saline during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poison A and B/
In a metabolism study /in rats/, 14C-isoxaflutole was rapidly and extensively absorbed and metabolized. ...Elimination was rapid and dose-dependent. The mean total recovery was 99.21%. Urinary eliminaton was predominant in the two low dose groups while the major portion of radiolabel was excreted via the feces in the high dose group. The higher fecal elimination possibly resulted from the saturation of absorption resulting in elimination of unchanged parent compound. The majority of the radiolabel was eliminated in the first 24 and 48 hours for the low and the high dose groups, respectively. The elimination half-lives were similar among single low and high dose groups, with an estimated mean blood half-life of 60 hours. No sex differences were observed in the metabolism of 14C-isoxaflutole.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
口服给药后，异草胺醌被迅速排出体外。
Following oral administration, isoxaflutole is rapidly excreted.
The absorption, distribution, metabolism and excretion of 14C-phenyl labelled isoxaflutole (14C-RPA 201772, purity >98%) was examined in Sprague-Dawley (SD) rats. For the single oral low- and high-dose groups, five animals/sex received a single dose of either 1 or 100 mg/kg bw of 14C-RPA 201772, respectively, by oral gavage. For the repeat oral low-dose, another 5 animals/sex received a nonradiolabelled low dose (1 mg/kg bw) for 14 consecutive days followed by a single dose of 1.0 mg/kg bw of 14C-RPA 201772 by oral gavage. For blood pharmacokinetic experiments another 5 animals/sex received a single dose of 1.0 or 100 mg/kg bw 14C-RPA 201772 by oral gavage. All animals were sacrificed at 168 hr post-dosing. RPA 201772 was rapidly absorbed at both 1.0 and 100 mg/kg bw. The maximal whole blood concentration was achieved within 1 hr at both dose levels. On the basis of available urinary excretion data (radioactivity detected in urine, cage washes and tissues) the mean estimated proportion of the administered dose absorbed was approximately 39, 73 and 75% for the high-, low- and repeat-dose groups, respectively. Tissue distribution of radioactivity between the sexes appeared to be similar. In the high-dose group, the highest levels in both sexes were found in the blood and plasma and to a lesser extent in the liver and kidneys of males and in the liver, kidneys, lungs and heart of females. In the single and repeat low-dose groups, higher tissue concentrations were found in the liver and kidneys. Elimination was rapid and dose dependent. The major route of elimination in the high-dose group was via the feces (approximately 55-63% of the administered dose) and in the single and repeat low-dose groups was via the urine (68-74% of the administered dose). The majority of the activity was eliminated within 24 and 48 hr post-dosing for the low- and high-dose groups, respectively. The terminal elimination phase T½ was about 60 hr in both sexes at both dose levels. Higher fecal elimination at the high dose may be due to saturation of absorption, resulting in elimination of unchanged parent compound. Mean recovery of radioactivity in the tissues at 168 hr post-dosing was low, indicating that there was most likely a good systemic clearance of the test substance with little potential for accumulation. RPA 201772 was rapidly and extensively metabolized. The major metabolite was the diketonitrile RPA 202248 (70-85% of the administered dose). Minor metabolites included RPA 203328 (0.6-3.6% of the administered dose), RPA 207048, RPA 205834 and RPA 205568. The parent compound, RPA 201772, was only detected in fecal extracts in the single high-dose group during the first 24 hr. Data suggest that only Phase I reactions occurred; there was no indication of any metabolites resulting from Phase II (conjugation) reactions. ... . The absorption, distribution, metabolism and excretion were not influenced by repeat oral administration.
The goats were dosed (balling gun) at a dietary burden of 10 ppm for seven days. The administered radioactivity was mainly eliminated via the urine and feces with the remaining radioactivity found in tissues, milk and cage wash and debris. Isoxaflutole was not identified in any of the tissues and milk. RPA 202248 was identified as a major component in all tissues, including milk. RPA 207048 was identified as a minor component in tissues and milk.
The herbicide isoxaflutole 1 (5-cyclopropyl-4-isoxazolyl)[2-(methylsulfonyl)-4-(trifluoromethyl)phenyl]- methanone) has been applied preemergence at the rate of 125 g ha(-1) on corn crops grown on fields located in regions different as to their soil textures. Its metabolite diketonitrile 2 (2-cyano-3-cyclopropyl- 1- (2-methylsulfonyl-4-trifluoromethylphenyl)propane- 1,3-dione)-which is the herbicide's active compound-and its nonherbicide metabolite 3 (2-methylsulfonyl-4-trifluoromethylbenzoic acid) were measured in the 0-10 cm surface soil layer of the corn crops after the treatment and until the harvest. At the opposite of what occurred in plant shoots, the transformation of isoxaflutole 1 into diketonitrile 2 was not immediate in soil. In the 0-10 cm surface soil layer, this transformation occurred progressively according to an apparent second-order kinetics, and the soil half-lives of isoxaflutole I self were comprised between 9 and 18 days. The adsorption of isoxaflutole I onto the solid phase of the soil and its organic matter should explain the stabilization effect of soil, increased by the application of fresh organic fertilizer. The sum of the concentrations of isoxaflutole I and diketonitrile 2 disappeared in the 0-10 cm surface soil layer according to an apparent first-order kinetics, and the soil half-lives of this sum were comprised between 45 and 65 days. The sum of the concentrations of isoxaflutole 1 and of its metabolites diketonitrile 2 and acid 3 did not account for the amount of isoxaflutole I applied. The discrepancy increased with the delay after the application, showing that the acid 3 was further metabolized in soil into common nontoxic products, and ultimately into CO2. The conjunction of the adsorption of isoxaflutole and its metabolites (which reduced their mobilities) onto the soil and its organic matter, and their further metabolism should explain why isoxaflutole and its metabolites were not detected in the 10-15 and 15-20 cm surface soil layers during the crops.
[EN] ACC INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE L'ACC ET UTILISATIONS ASSOCIÉES
申请人：GILEAD APOLLO LLC
公开号：WO2017075056A1
公开（公告）日：2017-05-04
The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
[EN] 3-[(HYDRAZONO)METHYL]-N-(TETRAZOL-5-YL)-BENZAMIDE AND 3-[(HYDRAZONO)METHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE DERIVATIVES AS HERBICIDES<br/>[FR] DÉRIVÉS DE 3-[(HYDRAZONO))MÉTHYL]-N-(TÉTRAZOL-5-YL)-BENZAMIDE ET DE 3-[(HYDRAZONO)MÉTHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE UTILISÉS EN TANT QU'HERBICIDES
申请人：SYNGENTA CROP PROTECTION AG
公开号：WO2021013969A1
公开（公告）日：2021-01-28
The present invention related to compounds of Formula (I): or an agronomically acceptable salt thereof, wherein Q, R2, R3, R4, R5 and R6 are as described herein. The invention further relates to compositions comprising said compounds, to methods of controlling weeds using said compositions, and to the use of compounds of Formula (I) as a herbicide.
[EN] INSECTICIDAL TRIAZINONE DERIVATIVES<br/>[FR] DÉRIVÉS DE TRIAZINONE INSECTICIDES
申请人：SYNGENTA PARTICIPATIONS AG
公开号：WO2013079350A1
公开（公告）日：2013-06-06
Compounds of the formula (I) or (I'), wherein the substituents are as defined in claim 1, are useful as pesticides.
式(I)或(I')的化合物，其中取代基如权利要求1所定义的那样，可用作杀虫剂。
[EN] HERBICIDALLY ACTIVE HETEROARYL-S?BSTIT?TED CYCLIC DIONES OR DERIVATIVES THEREOF<br/>[FR] DIONES CYCLIQUES SUBSTITUÉES PAR HÉTÉROARYLE À ACTIVITÉ HERBICIDE OU DÉRIVÉS DE CELLES-CI
申请人：SYNGENTA LTD
公开号：WO2011012862A1
公开（公告）日：2011-02-03
The invention relates to a compound of formula (I), which is suitable for use as a herbicide wherein G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or latentiating group; Q is a unsubstituted or substituted C3-C8 saturated or mono-unsaturated heterocyclyl containing at least one heteroatom selected from O, N and S, or Q is heteroaryl or substituted heteroaryl; m is 1, 2 or 3; and Het is an optionally substituted monocyclic or bicyclic heteroaromatic ring; and wherein the compound is optionally an agronomically acceptable salt thereof.
[EN] BENZOTHIAZOLE CARBOXAMIDES AS FUNGICIDES<br/>[FR] BENZOTHIAZOLE CARBOXAMIDES EN TANT QUE FONGICIDES
申请人：SUMITOMO CHEMICAL CO
公开号：WO2009157527A1
公开（公告）日：2009-12-30
An amide compound of the formula (I): (wherein, R1 represents a hydrogen atom or fluorine atom and R2 represents a C1 to C6 linear alkyl group or linear (C1-C2 alkoxy)C2-C5 alkyl group.) has an excellent controlling effect on a plant disease.
