4-氟-3-甲氧基苯肼盐酸盐 | 327021-81-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-氟-3-甲氧基苯肼盐酸盐
• 英文名称: (4-fluoro-3-methoxy-phenyl)hydrazine hydrochloride
• 英文别名: (4-Fluoro-3-methoxyphenyl)hydrazine hydrochloride；(4-fluoro-3-methoxyphenyl)hydrazine;hydrochloride
• CAS: 327021-81-8
• 化学式: C₇H₉FN₂O*ClH
• 分子量: 192.621
• InChiKey: DMOWKTFIFYPUQA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.54
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  47.3
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  4-氟-3-甲氧基苯肼盐酸盐 、 (NE)-3-bromo-N-[1-(dimethylamino)ethylidene]imidazo[1,2-a]pyridine-6-carboxamide 以 N,N-二甲基甲酰胺 为溶剂， 生成 3-bromo-6-[2-(4-fluoro-3-methoxy-phenyl)-5-methyl-1,2,4-triazol-3-yl]imidazo[1,2-a]pyridine
  参考文献：
  名称：

  IMIDAZO[1,2-A]PYRIDINE DERIVATIVES

  摘要：

  The current invention relates to compounds of the formula (I), wherein the substituents are as defined in claim 1, to processes and methods for preparing compounds of formula (I), to agrochemical compositions comprising compounds of formula (I) as defined in claim 1, to preparation of these compositions and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.

  公开号：

  WO2024126404A1
• 作为产物：
  描述：

  4-氟-3-甲氧基苯胺 在 盐酸 、 sodium nitrite 、 tin(ll) chloride 作用下， 以 水 为溶剂， 反应 5.33h， 以67%的产率得到4-氟-3-甲氧基苯肼盐酸盐
  参考文献：
  名称：

  Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application

  摘要：

  一种化学化合物的化学式（I），其中：R1和R2独立选择自氢和烷基；R3是烷基；R4、R6和R7独立选择自氢、卤素、羟基、烷基、芳基、氨基、烷基氨基、二烷基氨基、烷氧基、芳氧基、烷基硫基、烷基亚砜基、烷基磺基、硝基、碳氰基、羰基烷氧基、羰基芳氧基和羧基；R5选择自氢、卤素、羟基、烷基、芳基、氨基、烷基氨基、二烷基氨基、烷氧基、芳氧基、烷基硫基、烷基亚砜基、烷基磺基、硝基、碳氰基、羰基烷氧基、羰基芳氧基和羧基；A是一个5-或6-成员部分不饱和或芳香杂环环或一个5-或6-成员部分不饱和脂环环，如果A是一个6-成员部分不饱和脂环环，则R4至R7中至少一个不是氢，以及其在治疗中的使用，特别是作为5HT受体的激动剂或拮抗剂，特别是5HT2C受体，例如在治疗中枢神经系统疾病；中枢神经系统损伤；心血管疾病；胃肠疾病；尿崩症和睡眠呼吸暂停症，特别是用于肥胖症的治疗。

  公开号：

  US06706750B1

文献信息

• Tetracyclic indolines as a novel class of β-lactam-selective resistance-modifying agent for MRSA
  作者：Yugen Zhu、Lakota Cleaver、Wei Wang、Jessica D. Podoll、Shane Walls、Austin Jolly、Xiang Wang

  DOI：10.1016/j.ejmech.2016.09.034

  日期：2017.1

  marked increase in recent years, while antibiotic discovery has waned. Resistance-modifying agents (RMA) offer an intriguing alternative strategy to fight against resistant bacteria. Here we report the discovery, antibiotic profiling, and structure-activity relationships of a novel class of RMAs, tetracyclic indolines. These selectively potentiate β-lactam antibiotics in methicillin-resistant Staphylococcus

  近年来，对抗生素具有抗药性的细菌感染显着增加，而对抗生素的发现却有所减少。抗性改良剂（RMA）提供了一种有趣的替代策略来对抗抗性细菌。在这里，我们报告的发现，一类新型的RMA，四环吲哚啉的抗生素分析和结构活性关系。这些选择性增强了耐甲氧西林的金黄色葡萄球菌（MRSA）中的β-内酰胺抗生素，而没有抗菌或β-内酰胺酶抑制活性。最有效的类似物6a，显示出阿莫西林/克拉维酸在各种医院获得的和社区获得的具有低哺乳动物毒性的MRSA菌株中具有强大的增效作用。可以进一步开发这些化合物，以延长β-内酰胺类抗生素的临床寿命。
• Continuous Flow Process For the Synthesis of Phenylhydrazine Salts and Substituted Phenylhydrazine Salts
  申请人：SHANGHAI HYBRID-CHEM TECHNOLOGIES

  公开号：US20190152896A1

  公开（公告）日：2019-05-23

  The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.

  本发明提供了一种连续流程，用于合成苯肼盐和取代苯肼盐。重氮化、还原、酸性水解和酸化与酸类创新地集成在一起。使用苯胺或取代苯胺的酸性液体、重氮化试剂、还原剂和酸类作为原料，通过合成过程获得苯肼衍生物盐，这是一个包括重氮化、还原、酸性水解和酸化的三步连续串联反应。所述的合成过程是一种集成解决方案，是在一个集成反应器中进行的。集成反应器的进料口连续填充原料。在集成反应器中，重氮化、还原、酸性水解和酸化被连续有序地进行，苯肼盐或取代苯肼盐在集成反应器的出口处获得，没有中断。总反应时间不超过20分钟。
• SUBSTITUTED HETEROARYL DERIVATIVES
  申请人：Zemolka Saskia

  公开号：US20100009986A1

  公开（公告）日：2010-01-14

  The invention relates to substituted heteroaryl derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted heteroaryl derivatives for producing medicaments.

  这项发明涉及替代杂环芳基衍生物，涉及其生产方法，含有该化合物的药物以及利用替代杂环芳基衍生物生产药物的用途。
• Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application
  申请人：Vernalis Research Limited

  公开号：US06706750B1

  公开（公告）日：2004-03-16

  A chemical compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4, R6 and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsufoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R5 is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R4 to R7 is other than hydrogen, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof, and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinial disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

  一种化学化合物的化学式（I），其中：R1和R2独立选择自氢和烷基；R3是烷基；R4、R6和R7独立选择自氢、卤素、羟基、烷基、芳基、氨基、烷基氨基、二烷基氨基、烷氧基、芳氧基、烷基硫基、烷基亚砜基、烷基磺基、硝基、碳氰基、羰基烷氧基、羰基芳氧基和羧基；R5选择自氢、卤素、羟基、烷基、芳基、氨基、烷基氨基、二烷基氨基、烷氧基、芳氧基、烷基硫基、烷基亚砜基、烷基磺基、硝基、碳氰基、羰基烷氧基、羰基芳氧基和羧基；A是一个5-或6-成员部分不饱和或芳香杂环环或一个5-或6-成员部分不饱和脂环环，如果A是一个6-成员部分不饱和脂环环，则R4至R7中至少一个不是氢，以及其在治疗中的使用，特别是作为5HT受体的激动剂或拮抗剂，特别是5HT2C受体，例如在治疗中枢神经系统疾病；中枢神经系统损伤；心血管疾病；胃肠疾病；尿崩症和睡眠呼吸暂停症，特别是用于肥胖症的治疗。
• Indoline derivatives and method of treating obesity
  申请人：——

  公开号：US06479534B1

  公开（公告）日：2002-11-12

  The present invention relates to indoline derivatives. These compounds are especially useful for the prevention and treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes, sleep apnea, and especially for the treatment and prevention of obesity.

  本发明涉及吲哚啉衍生物。这些化合物特别适用于预防和治疗中枢神经系统紊乱；中枢神经系统损伤；心血管疾病；胃肠道疾病；糖尿病，睡眠呼吸暂停症，尤其是用于肥胖症的治疗和预防。