2-氟-5-甲氧基苯肼盐酸盐 | 1198283-29-2

• 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: 2-氟-5-甲氧基苯肼盐酸盐
• 英文名称: (2-fluoro-5-methoxyphenyl)hydrazine hydrochloride
• 英文别名: 2-fluoro-5-Methoxyphenylhydrazine hydrochloride；(2-fluoro-5-methoxyphenyl)hydrazine;hydrochloride
• CAS: 1198283-29-2
• 化学式: C₇H₉FN₂O*ClH
• 分子量: 192.621
• InChiKey: ZZUXPUUETOOTMQ-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

反应信息

• 作为反应物：
  描述：

  马来酸酐 、 2-氟-5-甲氧基苯肼盐酸盐 以 乙醇 为溶剂， 反应 24.0h， 以49%的产率得到1-(2-fluoro-5-methoxyphenyl)-1,2-dihydropyridazine-3,6-dione
  参考文献：
  名称：

  [EN] 2-ARYL- AND 2-HETEROARYL-SUBSTITUTED 2-PYRIDAZIN-3(2H)-ONE COMPOUNDS AS INHIBITORS OF FGFR TYROSINE KINASES
  [FR] COMPOSÉS DE 2-PYRIDAZIN-3(2H)-ONE À SUBSTITUTION 2-ARYLE ET 2-HÉTÉROARYLE UTILISÉS EN TANT QU'INHIBITEURS DE FGFR TYROSINE KINASES

  摘要：

  本文提供了一般式I的化合物及其立体异构体和药学上可接受的盐或溶剂，其中X、R1、R2、R3、环A和z的含义如规范中所述，这些化合物是FGFR1、FGFR2、FGFR3和/或FGFR4的抑制剂，可用于治疗和预防可以用FGFR抑制剂治疗的疾病，包括由FGFR1、FGFR2、FGFR3和/或FGFR4介导的疾病或障碍。

  公开号：

  WO2017070708A1

文献信息

• 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。
• Substituent effects on the isomerization of hydrazone switches driven by the intramolecular hydrogen bond
  作者：Chaocao Lu、Bu Htan、Shitao Fu、Chunmiao Ma、Quan Gan

  DOI：10.1016/j.tet.2019.06.022

  日期：2019.7

  In this work, the substituent effects on hydrogen bonding in one kind of hydrazone-based switch are revealed. The E/Z isomerization ratios of these hydrazones and their intramolecular hydrogen bond strengths in the Z form were evaluated using NMR technique. Linear correlations between these parameters and Hammett empirical values for substituent effects are explored as well.

  在这项工作中，揭示了一种基开关中取代基对氢键的影响。使用NMR技术评估这些的E / Z异构化比例及其在Z形式下的分子内氢键强度。还探讨了这些参数与Hammett经验值之间关于取代基效应的线性相关性。
• Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts
  申请人：SHANGHAI HYBRID—CHEM TECHNOLOGIES

  公开号：US11040938B2

  公开（公告）日：2021-06-22

  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.

  本发明提供了一种合成苯肼盐和取代苯肼盐的连续流工艺。重氮化、还原、酸性水解和酸盐化被创新性地整合在一起。以苯胺或取代苯胺的酸性液体、重氮化试剂、还原剂和酸为原料，通过重氮化、还原、酸性水解和盐化三步连续串联反应的合成工艺，获得苯肼衍生物盐。所述合成工艺是一种一体化解决方案，在一体化反应器中进行。集成反应器的进料口连续注入原料。在一体化反应器中，重氮化、还原、酸性水解和盐化连续有序地进行，在一体化反应器的出口处不间断地得到苯肼盐或取代苯肼盐。总反应时间不超过 20 分钟。