安美速 | 348635-87-0

• 物质功能分类: 分析化学 - 标准品 - 农业和环境标准品
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 中文名称: 安美速
• 中文别名: 吲唑磺菌胺；吲唑磺菌胺,100ΜG/ΜL于乙腈
• 英文名称: 3-[(3-bromo-6-fluoro-2-methyl-1H-indol-1-yl)sulfonyl]-N,N-dimethyl-1H-1,2,4-triazole-1-sulfonamide
• 英文别名: 3-((3-bromo-6-fluoro-2-methylindole-1-yl)-sulfonyl)-N,N-dimethyl-1,2,4-triazole-1-sulfonamide；3-(3-bromo-6-fluoro-2-methylindol-1-ylsulfonyl)-N,N-dimethyl-1H-1,2,4-triazole-1-sulfonamide；3-(3-bromo-6-fluoro-2-methylindol-1-ylsulfonyl)-N,N-dimethyl-1,2,4-triazole-1-sulfonamide；3-(3-bromo-6-fluoro-2-methylindole-1-sulfonyl)-N,N-dimethyl-1,2,4-triazole-1-sulfonamide；3-(3-bromo-6-fluoro-2-methylindol-1-ylsulfonyl)-1,2,4-triazole-1-sulfonyl-dimethylamine；amisuibrom；Amisulbrom；3-(3-bromo-6-fluoro-2-methylindol-1-yl)sulfonyl-N,N-dimethyl-1,2,4-triazole-1-sulfonamide
• CAS: 348635-87-0
• 化学式: C₁₃H₁₃BrFN₅O₄S₂
• 分子量: 466.312
• InChiKey: BREATYVWRHIPIY-UHFFFAOYSA-N

物化性质

• 熔点：
  128～132℃
• 沸点：
  651.5±65.0 °C(Predicted)
• 密度：
  1.85±0.1 g/cm3(Predicted)
• 溶解度：
  DMSO（少量）、甲醇（轻微、超声处理）
• LogP：
  1.980 (est)
• 颜色/状态：
  Fine powder
• 气味：
  Odorless
• 蒸汽压力：
  1.8X10-5 mPa /1.35X10-10 mm Hg/ at 25 °C

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  124
• 氢给体数：
  0
• 氢受体数：
  8

ADMET

代谢

在大鼠代谢研究中，韩威斯特大鼠接受了一次口服给药，剂量为10和1000毫克/千克的(吲哚-(14)C)或(三唑-(14)C)氨磺溴(放射性纯度>或=95.2%)，载体为水中的0.5%甲基纤维素。随后进行了一系列实验（每个剂量组4只/性别），评估每个剂量水平在给药后最多120小时内的放射性排泄和组织分布，并确定了血浆和全血的动力学。此外，还进行了一项实验，研究在单次口服给药10或1000毫克/千克的(吲哚-(14)C)NC-224后，从胆管插管的大鼠中排泄放射性物质。为了检查放射性物质在组织中的分布随时间的变化，大鼠还接受了10或1000毫克/千克的(吲哚-(14)C)氨磺溴的给药，然后在给药后2和24小时（10毫克/千克）或12和72小时（1000毫克/千克）处死了每个时间点的3只/性别的大鼠。对这些实验的排泄物和组织/器官样本进行了放射性分析，并对粪便、尿液、胆汁、肝脏和血浆的选定混合样本进行了分析，以确定代谢轮廓。...在两个性别的粪便中，母化合物是主要的(14)C残留物，占给药剂量的40-52%（10毫克/千克）和83-89%（1000毫克/千克）。从粪便、尿液和胆汁中分离出的其他组分/代谢物，每个组分占给药剂量的<5%，除了从低剂量大鼠胆汁中分离出的一个组分，占给药剂量的5.3%。这个组分暂时被识别为Metabolite IT-2的一种未特指的共轭物。除了母化合物外，尿液中还鉴定出了九种初级代谢物和一种代谢物的一种葡萄糖苷酸共轭物。其中两种代谢物（IT-4和IT-5）也被确定为肝脏（每个占肝脏总放射性残留物的12-20%；TRR in liver）和血浆（每个占血液中TRR的14-56%）在Tmax时的主要(14)C残留物。根据代谢轮廓，大鼠对氨磺溴的代谢涉及一系列反应，包括三唑环上磺酰氨基侧链的断裂，脱溴，氧化/羟基化，吲哚和三唑基团之间的磺酰桥有限的断裂，吲哚环的开启，以及初级代谢物的共轭。氨磺溴在大鼠中的主要代谢途径似乎涉及初始断裂磺酰氨基侧链以形成IT-4，随后羟基化为IT-5，然后这些初级代谢物进一步降解或共轭。

In a rat metabolism study, Han Wistar rats were treated with a single gavage dose of (indole- (14) C) or (triazole- (14)C) amisulbrom (radiochemical purity > or = 95.2%) at 10 and 1000 mg/kg in aqueous 0.5% methy1cellulose. A series of experiments were then performed (4/sex/dose group) evaluating the excretion and tissue distribution of radioactivity at each dose level at up to 120 hours post-dose, and plasma and whole blood kinetics were determined. An additional experiment was conducted examining the excretion of radioactivity from bile duct-cannulated rats following a single oral dose of (indole-(14)C) NC-224 at 10 or 1000 mg/kg. To examine the distribution of radioactivity in tissues over time, rats were also dosed with (indole- (14) C) amisulbrom at 10 or 1000 mg/kg and 3 rats/sex/time point were then sacrificed at 2 and 24 hours post-dose (10 mg/kg) or 12 and 72 hours post-dose (1000 mg/kg). Excreta and tissue/organ samples from these experiments were radioassayed, and selected pooled samples of feces, urine, bile, liver, and plasma were analyzed to determine the metabolic profile. ... Parent compound was the major (14)C-residue identified in feces of both sexes and (14)C-labels, accounting for 40-52% of the administered dose at 10 mg/kg and 83-89% at 1000 mg/kg. Other components/metabolites isolated from feces, urine and bile each accounted for <5% of the administered dose, with the exception of one component isolated from the bile of the low-dose rats that accounted for 5.3% of the administered dose. This component was tentatively identified as an unspecified conjugate of Metabolite IT-2. In addition to parent, nine primary metabolites and a glucuronide conjugate of one metabolite were identified in urine, feces and/or bile. Two of these metabolites (IT-4 and IT-5) were also identified as being the major (14)C-residues in liver (each 12-20% of the total radioactive residues; TRR in liver) and plasma (each 14-56% of the TRR in blood) at Tmax. Based on the metabolic profile, the metabolism of amisulbrom in the rat involves a series of reactions including cleavage of the sulfonyl amino side chain on the triazole ring, debromination, oxidation/hydroxylation, limited cleavage of the sulfonyl bridge between the indole and triazole moieties, indole ring opening, and conjugation of primary metabolites. The major route of metabolism of amisulbrom in rats appears to involve the initial cleavage of the sulfonylamino side to form IT-4 and it subsequent hydroxylation to IT-5, followed by further degradation or conjugation of these primary metabolites.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 立即急救：确保已经进行了充分的中和。如果患者停止呼吸，请开始人工呼吸，最好使用需求阀复苏器、球囊阀面罩设备或口袋面罩，按训练操作。如有必要，执行心肺复苏。立即用缓慢流动的水冲洗受污染的眼睛。不要催吐。如果患者呕吐，让患者向前倾或将其置于左侧（如果可能的话，头部向下）以保持呼吸道畅通，防止吸入。保持患者安静，维持正常体温。寻求医疗救助。 /毒物A和B/

/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 基本治疗：建立专利气道（如有需要，使用口咽或鼻咽气道）。如有必要，进行吸痰。观察呼吸不足的迹象，如有需要，辅助通气。通过非循环呼吸面罩以10至15升/分钟的速度给予氧气。监测肺水肿，如有必要，进行治疗……。监测休克，如有必要，进行治疗……。预防癫痫发作，如有必要，进行治疗……。对于眼睛污染，立即用水冲洗眼睛。在运输过程中，用0.9%的生理盐水（NS）持续冲洗每只眼睛……。不要使用催吐剂。对于摄入，如果患者能吞咽、有强烈的干呕反射且不流口水，则用温水冲洗口腔，并给予5毫升/千克，最多200毫升的水进行稀释……。在去污后，用干燥的无菌敷料覆盖皮肤烧伤……。/毒药A和B/

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). 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 0.9% saline (NS) 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 ... . /Poisons A and B/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 高级治疗：对于无意识、严重肺水肿或严重呼吸困难的病人，考虑进行口咽或鼻咽气管插管以控制气道。使用气囊面罩装置的正压通气技术可能有益。考虑使用药物治疗肺水肿……。对于严重的支气管痉挛，考虑给予β激动剂，如沙丁胺醇……。监测心率和必要时治疗心律失常……。开始静脉输注D5W /SRP: "保持开放"，最低流量/。如果出现低血容量的迹象，使用0.9%生理盐水（NS）或乳酸林格氏液。对于伴有低血容量迹象的低血压，谨慎给予液体。注意液体过载的迹象……。使用地西泮或劳拉西泮治疗癫痫……。使用丙美卡因氢氯化物协助眼部冲洗……。 /Poisons A and B/

/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 非人类毒性摘录

实验室动物：亚慢性或前慢性暴露/ 在一项亚慢性口服毒性研究中，将Amisulbrom（98.7% ai）以0、800、2500或8000 ppm的剂量水平（相当于0/0、118.8/163.4、400.3/505.6和1280.2/1638.4 mg/kg/天（M/F））通过饲料给予10只CD-1小鼠/性别/剂量，持续长达13周。这项研究的目的是帮助选择相关致癌性研究的剂量。在2500和8000 ppm剂量组的雌性小鼠中，观察到体重下降和整体（第0-13周）体重增加减少以及食物效率下降。在2500和8000 ppm剂量组中，相对于体重的肝脏重量在雄性和雌性中都有所增加。此外，在8000 ppm剂量组的雄性中，绝对肝脏重量也有所增加。这些增加不到30%。临床化学检查结果没有提供不良影响的证实证据。没有进行组织病理学检查。基于雌性体重增加减少和两性食物效率下降以及肝脏重量增加，最低观察到不良效应水平（LOAEL）为2500 ppm（相当于400/506 mg/kg/天（M/F））。没有观察到不良效应的剂量水平（NOAEL）为800 ppm（相当于119/163 mg/kg/天（M/F））。

/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ In a subchronic oral toxicity study Amisulbrom (98.7% ai) was administered to 10 CD-l mice/sex/dose in the diet at dose levels of 0, 800, 2500, or 8000 ppm (equivalent to 0/0, 118.8/163.4,400.3/505.6, and 1280.2/1638.4 mg/kg/day (M/F), respectively) for up to 13 weeks. The purpose of this study was to aid in the selection of doses for an associated carcinogenicity study. In the 2500 and 8000 ppm females, decreased body weights and overall (Weeks 0-13) body weight gains and decreased food efficiency were noted. At 2500 and 8000 ppm, relative (to body) liver weights were increased in the males and females. Additionally, absolute liver weight was increased in the 8000 ppm males. These increases were less than 30%. Clinical chemistry findings did not provide corroborating evidence of an adverse effect. Histopathological examinations were not performed. The LOAEL is 2500 ppm (equivalent to 400/506 mg/kglday [M/F]) based on decreases in body weight gain in the females and food efficiency in both sexes and liver weight increases were noted. The NOAEL is 800 ppm (equivalent to 119/163 mg/kg/day (M/F)).

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 非人类毒性摘录

实验室动物：亚慢性或前慢性暴露/在/a/亚慢性口服毒性研究中，给4只/性别/剂量的比格犬口服 amisulbrom（98.7% a.i），剂量为0、100、300或1000 mg/kg/天，连续13周。在死亡率、临床体征、眼科检查、血液学、临床化学、尿液分析、器官重量或大体或显微镜下病理学方面，未观察到与治疗相关的有害影响。在初始（前几周）期间，两性的体重增加和食物消耗都有短暂的减少。这种短暂的影响被认为不是有害的。在300和1000 mg/kg/天剂量的雄性（每组3/4）的肺和支气管上发现了苍白区域，但在对照组中只有一个。在100（1/4）、300（2/4）和1000（3/4）mg/kg/天剂量的雄性肺和支气管的肺下膜间隔中观察到最小到轻微的纤维化，但在对照组中未见到。根据这些观察结果，选择了100 mg/kg/天的LOAEL（最低观察到有害效应水平）。由于在最低测试剂量下就注意到了肺部影响，因此没有建立NOAEL（无观察到有害效应水平）。

/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ In /a/ subchronic oral toxicity study, amisulbrom (98.7% a.i) was administered to 4 beagle dogs/sex/dose for 13 weeks at doses of 0, 100, 300, or 1000 mg/kg/day orally by capsule. No adverse, treatment related effect was observed on mortality, clinical signs, ophthalmoscopic evaluations, hematology, clinical chemistry, urinalysis, organ weights, or gross or microscopic pathology. Initial (first few weeks) transient decreases in body weight gain and food consumption were noted in both sexes. This transient effect was not considered adverse. Pale area(s) were noted on the lungs and bronchi of the 300 and 1000 mg/kg/day males (3/4 each group) but in only one control. Minimal to slight subpleural septal fibrosis was observed in the lungs and bronchi of males at 100 (1/4), 300 (2/4) and 1000 (3/4) mg/kg/day but not seen in the controls. Based on these observations, a study LOAEL of 100 mg/kg/day was selected. No study NOAEL was established since the lung effects were noted at the lowest dose tested.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在大鼠代谢研究中，汉威斯特大鼠接受了一次口服剂量为10和1000毫克/千克的（吲哚-（14）C）或（三唑-（14）C）的 amisulbrom（放射性纯度>或=95.2%）的水溶液0.5%甲基纤维素。随后进行了一系列实验（每个剂量组4只/性别），评估每个剂量水平在给药后最多120小时内的放射性排泄和组织分布，并确定了血浆和全血的动力学。对单次口服剂量为10或1000毫克/千克的（吲哚-(14)C）NC-224的大鼠进行了额外的实验，以研究从胆管插管的大鼠中放射性物质的排泄。为了研究放射性物质随时间在组织中的分布，大鼠还接受了10或1000毫克/千克的（吲哚-（14）C）amisulbrom的剂量，然后在2和24小时后（10毫克/千克）或12和72小时后（1000毫克/千克）对每性别的3只大鼠进行安乐死。从这些实验中收集的排泄物和组织/器官样本进行了放射性分析，并分析了粪便、尿液、胆汁、肝脏和血浆的选定混合样本，以确定代谢轮廓。在初步研究中，呼出的空气中的放射性物质未被检测到。给药剂量为10和1000毫克/千克时，放射性物质的总体回收率为90-108%，两种（14）C标记物的性别排泄模式相似。粪便排泄是消除的主要途径。对于10毫克/千克剂量组，粪便排泄占给药剂量的80-98%，而尿液占10-14%。给药后120小时，残留在尸体和组织中的放射性物质占<0.5%。对于1000毫克/千克剂量组，粪便排泄占给药剂量的89-100%，尿液占1-3%，给药后120小时残留在尸体中的放射性物质占0.05%。在两个剂量水平上，大部分排泄发生在给药后0-48小时内。胆管插管大鼠的总体回收率为92-97%，吸收和排泄模式在性别之间相似。来自胆管插管大鼠的数据表明，10毫克/千克时，49-50%的给药剂量从胃肠道吸收；然而，相比之下，在1000毫克/千克的剂量水平上，只有5%的给药剂量被吸收，这表明在高剂量时胃肠道吸收已饱和。在10毫克/千克剂量组中，胆汁排泄占给药剂量的40-41%，44%的给药剂量未吸收的试验物质随粪便排出。尿液中只有9%的给药剂量。在1000毫克/千克剂量下，粪便占给药剂量的85-86%，胆汁和尿液各占1-3%。10毫克/千克组的血浆最大浓度（Tmax）发生在给药后2-6小时，1000毫克/千克组在6-12小时后，10毫克/千克组的最大血浆浓度（Cmax）为2-6 Ilg等效物/克，1000毫克/千克组为12-30 Ilg等效物/克。10毫克/千克的消除半衰期为18-35小时，1000毫克/千克的消除半衰期为8-13小时。对于三唑标记物，特别是在1000毫克/千克剂量组中，Tmax延迟。在所有时间点，组织中（14）C残留物的浓度（不包括GI tract）通常在肝脏中最高，其次是肾脏，组织中（14）C残留物的分布通常在性别之间相似。残留物水平随剂量增加而增加，但增加与剂量水平的增加不成比例。到给药后120小时，只有少量放射性物质（0.5%的给药剂量）在少数器官中可被检测到，如肾脏和肝脏。

In a rat metabolism study, Han Wistar rats were treated with a single gavage dose of (indole- (14)C) or (triazole- (14)C) amisulbrom (radiochemical purity > or = 95.2%) at 10 and 1000 mg/kg in aqueous 0.5% methy1cellulose. A series of experiments were then performed (4/sex/dose group) evaluating the excretion and tissue distribution of radioactivity at each dose level at up to 120 hours post-dose, and plasma and whole blood kinetics were determined. An additional experiment was conducted examining the excretion of radioactivity from bile duct-cannulated rats following a single oral dose of (indole-(14)C) NC-224 at 10 or 1000 mg/kg. To examine the distribution of radioactivity in tissues over time, rats were also dosed with (indole- (14) C) amisulbrom at 10 or 1000 mg/kg and 3 rats/sex/time point were then sacrificed at 2 and 24 hours post-dose (10 mg/kg) or 12 and 72 hours post-dose (1000 mg/kg). Excreta and tissue/organ samples from these experiments were radioassayed, and selected pooled samples of feces, urine, bile, liver, and plasma were analyzed to determine the metabolic profile. Radioactivity was not detectable in expired air in a preliminary study. The overall recovery of the radioactivity was 90-108% of the administered dose for both the 10 and 1000 mg/kg doses, and the pattern of excretion was similar between sexes for the two (14)C-labels. Fecal excretion was the major route of elimination. For the 10 mg/kg dose groups, fecal excretion accounted for 80-98% of the administered dose, while urine accounted for 10-14%. Radioactivity remaining in the carcass and tissues at 120 hours post-dose accounted for <0.5%. For the 1000 mg/kg dose groups, fecal excretion accounted for 89-100% of the administered dose, urine accounted for 1-3% of the administered dose, and radioactivity remaining in the carcass at 120 hours post-dose accounted for 0.05%. At both dose levels, the majority of excretion occurred from 0-48 hours post-dose. The overall total recovery from bile duct cannulated rats was 92-97% of the administered dose, and the patterns of absorption and excretion were similar between sexes. Data from the bile duct cannulated rats indicate that 49-50% of the administered dose was absorbed from the gastro-intestinal tract at 10 mg/kg; however, in contrast, only 5% of the administered dose was absorbed at the 1000 mg/kg dose level, indicating that gastro-intestinal absorption was saturated at the high dose. In the 10 mg/kg dose group, biliary excretion accounted for 40-41 % of the administered dose and 44% of the administered dose was unabsorbed test material eliminated in the feces. Only 9% of the administered dose was in the urine. At the 1000 mg/kg dose, feces accounted for 85-86% of the administered dose, and bile and urine each accounted for 1-3% of the administered dose. The time to maximum concentration in plasma (T max) occurred at 2-6 hours post -dose for the 10 mg/kg groups and 6-12 post-hours in the 1000 mg/kg group, and maximum plasma concentrations (Cmax) were 2-6 Ilg equiv./g for the 10 mg/kg group and 12-30 Ilg equiv./g in the 1000 mg/kg group. The elimination half-life was 18-35 hours at 10 mg/kg and 8-13 hours at 1000 mg/kg. For the triazole labeled material the T max was delayed especially at the 1000 mg/kg dose group. At all the time points, the concentrations of (14)C-residues in tissues (excluding the GI tract) were typically highest in liver followed by kidneys, and the distribution of (14)C-residues among tissues was generally similar between sexes. Residue levels increased with dose, but the increases were not proportional to the increase in the dose level. By 120 hours post-dose, only minor amounts of radioactivity "0.5% administered dose) were detectable in a few organs, such as kidneys and liver.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险品标志：
  N
• 安全说明：
  S61
• 危险类别码：
  R50
• WGK Germany：
  3

制备方法与用途

杀菌剂：杀菌剂——吲唑磺菌胺（Amisulbrom）

吲唑磺菌胺（安美速，Amisulbrom）是由日本日产化学公司于2003年研发的一种三唑磺酰胺类杀菌剂。它对由卵菌门真菌引起的病害表现出极高的活性，尤其在防控十字花科蔬菜根肿病方面表现优异，是一款以预防为主的杀菌剂。

杀菌作用机理

吲唑磺菌胺是一种三唑磺酰胺类触杀型杀菌剂，属于Qi(泛醌还原酶)位点真菌呼吸抑制剂。其主要通过抑制真菌的泛醌还原酶（Qi），阻断真菌的呼吸链，从而导致真菌死亡。此外，通过干扰真菌细胞膜结构和功能，增加细胞膜通透性，使细胞内物质外泄，进一步加速真菌细胞的死亡。

防治对象

吲唑磺菌胺对由卵菌纲引起的植物疫病和霜霉病具有较高的活性，特别是对游离孢子表现出极高的活性。它是一种以预防为主的药剂，可用于以下作物的病害防控：

• 茄科（马铃薯、烟草、辣椒、番茄）疫病
• 葡萄霜霉病
• 葫芦科作物（西葫芦、黄瓜、西瓜等）霜霉病
• 芸薹属（十字花科）作物根肿病
• 水稻立枯病
• 烟草黑胫病
• 草坪枯萎病
• 大姜根腐病

合成方法

吲唑磺菌胺的合成路线如下：

反应信息

• 作为产物：
  描述：

  3-bromo-6-fluoro-2-methyl indole 、 1-(N,N-dimethylaminosulfonyl)-1H-1,2,4-triazole-3-sulfonyl chloride 在 sodium hydroxide 、 四丁基溴化铵 、 水 作用下， 以 甲苯 为溶剂， 反应 7.0h， 以95%的产率得到安美速
  参考文献：
  名称：

  WO2006/57354

  摘要：

  公开号：

文献信息

• [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.

  本发明提供了化合物I和II，这些化合物可用作乙酰辅酶A羧化酶（ACC）的抑制剂，以及它们的组合物和使用方法。
• [EN] BICYCLYL-SUBSTITUTED ISOTHIAZOLINE COMPOUNDS<br/>[FR] COMPOSÉS ISOTHIAZOLINE SUBSTITUÉS PAR UN BICYCLYLE
  申请人：BASF SE

  公开号：WO2014206910A1

  公开（公告）日：2014-12-31

  The present invention relates to bicyclyl-substituted isothiazoline compounds of formula (I) wherein the variables are as defined in the claims and description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.

  本发明涉及公式（I）中变量如索权和说明中所定义的自行车基取代异噻唑啉化合物。这些化合物对抗或控制无脊椎动物害虫，特别是节肢动物害虫和线虫方面具有用途。该发明还涉及一种通过使用这些化合物来控制无脊椎动物害虫的方法，以及包含所述化合物的植物繁殖材料、农业和兽医组合物。
• [EN] AZOLINE COMPOUNDS<br/>[FR] COMPOSÉS AZOLINE
  申请人：BASF SE

  公开号：WO2015128358A1

  公开（公告）日：2015-09-03

  The present invention relates to azoline compounds of formula (I) wherein A, B1, B2, B3, G1, G2, X1, R1, R3a, R3b, Rg1 and Rg2 are as defined in the claims and the description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.

  本发明涉及式（I）的噁唑啉化合物，其中A、B1、B2、B3、G1、G2、X1、R1、R3a、R3b、Rg1和Rg2如权利要求和描述中所定义。这些化合物对抗或控制无脊椎动物害虫，特别是节肢动物害虫和线虫方面具有用途。该发明还涉及一种利用这些化合物控制无脊椎动物害虫的方法，以及包括所述化合物的植物繁殖材料、农业和兽医组合物。
• [EN] SUBSTITUTED QUINAZOLINES AS FUNGICIDES<br/>[FR] QUINAZOLINES SUBSTITUÉES, UTILISÉES EN TANT QUE FONGICIDES
  申请人：SYNGENTA PARTICIPATIONS AG

  公开号：WO2010136475A1

  公开（公告）日：2010-12-02

  The present invention relates to a compound of formula (I) wherein wherein the substituents have the definitions as defined in claim 1or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.

  本发明涉及一种具有如下式（I）的化合物，其中取代基具有权利要求1中定义的定义，或其盐或N-氧化物，它们的用途以及用于控制和/或预防植物中微生物感染，特别是真菌感染的方法，以及制备这些化合物的方法。
• [EN] MICROBIOCIDAL OXADIAZOLE DERIVATIVES<br/>[FR] DÉRIVÉS D'OXADIAZOLE MICROBIOCIDES
  申请人：SYNGENTA PARTICIPATIONS AG

  公开号：WO2017157962A1

  公开（公告）日：2017-09-21

  Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially fungicides.

  式(I)的化合物，其中取代基如权利要求1所定义，作为杀虫剂特别是杀菌剂有用。