3-氟-4-羟基-N-甲基-苯甲酰胺 | 633317-77-8

• 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: 3-氟-4-羟基-N-甲基-苯甲酰胺
• 英文名称: 3-fluoro-4-hydroxy-N-methylbenzamide
• CAS: 633317-77-8
• 化学式: C₈H₈FNO₂
• 分子量: 169.155
• InChiKey: KNBPKLKCNUCTCC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-氟-4-羟基-N-甲基-苯甲酰胺 、 三氟甲烷磺酸甲酯 生成
  参考文献：
  名称：

  4-Methyl-5-phenyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type I

  摘要：

  4-Methyl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1). They were active in vitro and in an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.04.013
• 作为产物：
  描述：

  4-(benzyloxy)-3-fluoro-N-methylbenzamide 在 palladium 10% on activated carbon 氢气 作用下， 以 乙醇 、 水 为溶剂， 20.0 ℃ 、344.75 kPa 条件下， 反应 64.0h， 以93%的产率得到3-氟-4-羟基-N-甲基-苯甲酰胺
  参考文献：
  名称：

  [EN] 4- (5-CYANO-PYRAZOL-1-YL) -PIPERIDINE DERIVATIVES AS GPR 119 MODULATORS
  [FR] DÉRIVÉS DE 4-(5-CYANOPYRAZOL-1-YL)PIPÉRIDINE EN TANT QUE MODULATEURS DU GPR119

  摘要：

  本文描述了调节G蛋白偶联受体GPR119活性的化合物及其在治疗与动物中G蛋白偶联受体GPR119调节相关疾病中的用途。

  公开号：

  WO2012069948A1

文献信息

• [EN] NEW ANTIFIBRINOLYTIC COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS ANTIFIBRINOLYTIQUES
  申请人：PROYECTO BIOMEDICINA CIMA SL

  公开号：WO2014012964A1

  公开（公告）日：2014-01-23

  It relates to spirocyclic compounds of formula (I),or pharmaceutically or veterinary acceptable salts thereof, or any stereoisomers either of the compounds of formula (I) or of their pharmaceutically or veterinary acceptable salts, wherein A and B form a spirocyclic ring system wherein the spiro atom connecting A and B is a carbonatom and wherein A is a known 3- to 8-membered carbocyclic or heterocyclic monocyclic ring or a known 6- to 18-membered carbocyclic or heterocyclic polycyclic ring system; B is a known 4- to 7-membered carbocyclic or heterocyclic monocyclic ring; C is phenyl or a known 5- to 6-membered heteroaromatic ring; and R1-R7 are as defined herein. It also relates to a process for their preparation, as well as to the intermediates used in this process; to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular as antifibrinolytic and antihemorragic agents.

  这涉及到公式(I)的螺环化合物，或其在药用或兽医学上可接受的盐，或者公式(I)化合物或其药用或兽医学上可接受的盐的立体异构体，其中A和B形成一个螺环系统，其中连接A和B的螺原子是一个碳原子，A是已知的3-至8-成员碳环或杂环单环，或已知的6-至18-成员碳环或杂环多环系统；B是已知的4-至7-成员碳环或杂环单环；C是苯基或已知的5-至6-成员杂芳环；R1-R7如此定义。它还涉及到它们的制备方法，以及在该过程中使用的中间体；含有它们的药用或兽医学组合物，以及它们在医学中的用途，特别是作为抗纤溶和抗出血剂。
• NEW ANTIFIBRINOLYTIC COMPOUNDS
  申请人：PROYECTO DE BIOMEDICINA CIMA, S.L.

  公开号：US20150175618A1

  公开（公告）日：2015-06-25

  It relates to spirocyclic compounds of formula (I), or pharmaceutically or veterinary acceptable salts thereof, or any stereoisomers either of the compounds of formula (I) or of their pharmaceutically or veterinary acceptable salts, wherein A and B form a spirocyclic ring system wherein the spiro atom connecting A and B is a carbon atom and wherein A is a known 3- to 8-membered carbocyclic or heterocyclic monocyclic ring or a known 6- to 18-membered carbocyclic or heterocyclic polycyclic ring system; B is a known 4- to 7-membered carbocyclic or heterocyclic monocyclic ring; C is phenyl or a known 5- to 6-membered heteroaromatic ring; and R 1 -R 7 are as defined herein. It also relates to a process for their preparation, as well as to the intermediates used in this process; to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular as antifibrinolytic and antihemorragic agents.

  本发明涉及公式(I)的螺环化合物，或其药学或兽医可接受的盐，或任何化合物的立体异构体(I)或其药学或兽医可接受的盐，其中A和B形成一个螺环系统，其中连接A和B的螺原子是一个碳原子，其中A是已知的3-8个成员的碳环或杂环单环或已知的6-18个成员的碳环或杂环多环系统；B是已知的4-7个成员的碳环或杂环单环；C是苯或已知的5-6个成员的杂芳环；R1-R7如本文所定义。本发明还涉及制备它们的方法，以及用于该过程中使用的中间体；包含它们的药学或兽医组合物，并将其用于医学，特别是作为抗纤溶和抗出血剂。
• [EN] 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS USEFUL FOR THE TREATMENT OF DIABETES, OBESITY AND DYSLIPIDEMIA<br/>[FR] INHIBITEURS DE LA 11-BETA-HYDROXYSTEROIDE DESHYDROGENASE 1 UTILISABLES POUR LE TRAITEMENT DU DIABETE, DE L'OBESITE ET DE LA DYSLIPIDEMIE
  申请人：——

  公开号：WO2003104207A3

  公开（公告）日：2004-03-25
• Discovery of a small molecule inhibitor through interference with the gp120–CD4 interaction
  作者：David H. Williams、Fiona Adam、David R. Fenwick、Juin Fok-Seang、Iain Gardner、Duncan Hay、Rawal Jaiessh、Donald S. Middleton、Charles E. Mowbray、Tanya Parkinson、Manos Perros、Christopher Pickford、Michelle Platts、Amy Randall、Daniel Siddle、Peter T. Stephenson、Thien-Duc Tran、Hannah Vuong

  DOI：10.1016/j.bmcl.2009.06.080

  日期：2009.9

  A series of piperazine derivatives were designed and synthesised as gp120-CD4 inhibitors. SAR studies led to the discovery of potent inhibitors in a cell based anti viral assay represented by compounds 9 and 28. The rat pharmacokinetic and antiviral profiles of selected compounds are also presented. Crown Copyright (C) 2009 Published by Elsevier Ltd. All rights reserved.
• 11-beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP1532122B1

  公开（公告）日：2011-12-14