rac-2-amino-4,4,4-trifluorobutan-1-ol | 497165-91-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: rac-2-amino-4,4,4-trifluorobutan-1-ol
• 英文别名: 2-amino-4,4,4-trifluorobutan-1-ol；2-amino-4,4,4-trifluorbutan-1-ol；2-amino-4,4,4-trifluoro-1-Butanol
• CAS: 497165-91-0
• 化学式: C₄H₈F₃NO
• mdl: MFCD19205712
• 分子量: 143.109
• InChiKey: CYRIDDDXXMMLMU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  氯甲酸苄酯 、 rac-2-amino-4,4,4-trifluorobutan-1-ol 在 potassium carbonate 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 2.5h， 以490 mg的产率得到rac-benzyl (4,4,4-trifluoro-1-hydroxybutan-2-yl)carbamate
  参考文献：
  名称：

  Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use

  摘要：

  本申请涉及新型取代咪唑[1,2-a]吡啶-3-羧酰胺，其制备方法，单独或组合使用以治疗和/或预防疾病，以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管疾病。

  公开号：

  US20140128372A1
• 作为产物：
  描述：

  2-氨基-4,4,4-三氟丁酸 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 反应 1.0h， 生成 rac-2-amino-4,4,4-trifluorobutan-1-ol
  参考文献：
  名称：

  [EN] BICYCLIC JAK INHIBITORS AND USES THEREOF
  [FR] INHIBITEURS DE JAK BICYCLIQUES ET LEURS UTILISATIONS

  摘要：

  本文提供了公式（I）、（II）、（III）和（IV）及其子公式的化合物，其中变量在此处定义。本文还提供了包括公式（I）、（II）、（III）或（IV）化合物的药物组合物，以及使用这些化合物的方法，例如用于治疗免疫紊乱、炎症性疾病和癌症。

  公开号：

  WO2020198583A1

文献信息

• Hydroxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20140128386A1

  公开（公告）日：2014-05-08

  The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

  本申请涉及新型取代咪唑[1,2-a]吡啶-3-羧酰胺，以及它们的制备方法，单独或组合使用于治疗和/或预防疾病，以及用于制备用于治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管疾病。
• Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof
  申请人：Wyeth

  公开号：US20040198778A1

  公开（公告）日：2004-10-07

  Compounds of Formula (I), 1 are provided where T is CHO, CON, or C(OH)R 1 R 2 ; R 1 and R 2 are hydrogen, optionally substituted lower alkyl, CF 3 , optionally substituted alkenyl, or optionally substituted alkynyl; R 3 is hydrogen or optionally substituted lower alkyl; R 4 is (CF 3 ) n alkyl, (CF 3 ) n (substitutedalkyl), (CF 3 ) n alkylphenyl, (CF 3 ) n alkyl(substitutedphenyl), or (F) n cycloalkyl; n=1-3; R 5 is hydrogen, halogen, CF 3 , diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR 6 or N where at least one of W, Y or Z are C; R 6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO 2 , or NR 7 ; R 7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R 8 is lower alkyl, CF 3 , or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

  提供了具有式(I)的化合物，其中T为CHO、CON或C(OH)R1R2；R1和R2为氢、可选择取代的较低烷基、CF3、可选择取代的烯烃或可选择取代的炔烃；R3为氢或可选择取代的较低烷基；R4为( )n烷基、( )n(取代烷基)、( )n烷基苯基、( )n烷基(取代苯基)或(F)n环烷基；n=1-3；R5为氢、卤素、 、与Y融合的双烯烃（当Y为C时）、或与Y融合的取代双烯烃（当Y为C时）；W、Y和Z为C、CR6或N，其中至少有一个为C；R6为氢、卤素或可选择取代的较低烷基；X为O、S、SO2或NR7；R7为氢、可选择取代的较低烷基、可选择取代的苄基或可选择取代的苯基；R8为较低烷基、 或可选择取代的苯基。还描述了制备和使用这些化合物来抑制β淀粉样蛋白的产生，以及治疗阿尔茨海默病和唐氏综合征的方法。
• FLUORO- AND TRIFLUOROALKYL-CONTAINING HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION AND DERIVATIVES THEREOF
  申请人：Kreft Anthony Frank

  公开号：US20090227667A1

  公开（公告）日：2009-09-10

  Compounds of Formula (I), are provided where T is CHO, COR 8 , or C(OH)R 1 R 2 ; R 1 and R 2 are hydrogen, optionally substituted lower alkyl, CF 3 , optionally substituted alkenyl, or optionally substituted alkynyl; R 3 is hydrogen or optionally substituted lower alkyl; R 4 is (CF 3 ) n alkyl, (CF 3 ) n (substitutedalkyl), (CF 3 ) n alkylphenyl, (CF 3 ) n alkyl(substitutedphenyl), or (F) n cycloalkyl; n=1-3; R 5 is hydrogen, halogen, CF 3 , diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR 6 or N where at least one of W, Y or Z are C; R 6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO 2 , or NR 7 ; R 7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R 8 is lower alkyl, CF 3 , or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

  提供了化学式（I）的化合物，其中T为CHO，COR8或C（OH）R1R2; R1和R2为氢，可选取代的低级烷基，CF3，可选取代的烯基或可选取代的炔基; R3为氢或可选取代的低级烷基; R4为（ ）n烷基，（ ）n（取代烷基），（ ）n烷基苯基，（ ）n烷基（取代苯基）或（F）n环烷基; n = 1-3; R5为氢，卤素， ，与Y融合的二烯或与Y融合的取代二烯，当Y = C时; W，Y和Z为C，CR6或N，其中至少有一个为C; R6为氢，卤素或可选取代的低级烷基; X为O，S，SO2或NR7; R7为氢，可选取代的低级烷基，可选取代的苄基或可选取代的苯基; R8为低级烷基， 或可选取代的苯基。还描述了制备和使用这些化合物来抑制β淀粉样蛋白生成以及治疗阿尔茨海默病和唐氏综合症的方法。
• Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof
  申请人：Kreft Frank Anthony

  公开号：US20070254929A1

  公开（公告）日：2007-11-01

  Compounds of Formula (I), are provided where T is CHO, COR 8 , or C(OH)R 1 R 2 ; R 1 and R 2 are hydrogen, optionally substituted lower alkyl, CF 3 , optionally substituted alkenyl, or optionally substituted alkynyl; R 3 is hydrogen or optionally substituted lower alkyl; R 4 is (CF 3 ) n alkyl, (CF 3 ) n (substitutedalkyl), (CF 3 ) n alkylphenyl, (CF 3 ) n alkyl(substitutedphenyl), or (F) n cycloalkyl; n=1-3; R 5 is hydrogen, halogen, CF 3 , diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR 6 or N where at least one of W, Y or Z are C; R 6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO 2 , or NR 7 ; R 7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R 8 is lower alkyl, CF 3 , or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

  提供了式(I)的化合物，其中T为CHO，COR8或C(OH)R1R2；R1和R2为氢，可选取代的低烷基，CF3，可选取代的烯基或可选取代的炔基；R3为氢或可选取代的低烷基；R4为( )n烷基，( )n（取代烷基），( )n烷基苯基，( )n烷基（取代苯基）或(F)ncycloalkyl；n=1-3；R5为氢，卤素， ，当Y═C时，为融合到二烯基，或当Y═C时，为取代的融合二烯基；W，Y和Z为C，CR6或N，其中至少有一个为C；R6为氢，卤素或可选取代的低烷基；X为O，S，SO2或NR7；R7为氢，可选取代的低烷基，可选取代的苯甲基或可选取代的苯基；R8为低烷基， 或可选取代的苯基。还描述了制备和使用这些化合物来抑制β淀粉样蛋白的产生以及治疗阿尔茨海默病和唐氏综合症的方法。
• Cgrp Receptor Antagonists
  申请人：Burgey Christopher S.

  公开号：US20080113966A1

  公开（公告）日：2008-05-15

  Compounds of Formula (I): and Formula (II): (where variables R 2 , R 4 , A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

  式(I)和式(II)的化合物(其中变量R2、R4、A、B、D、W、X、Y和Z的定义如本文所述)，可用作CGRP受体拮抗剂，用于治疗或预防CGRP参与的疾病，如头痛、偏头痛和集群头痛。本发明还涉及包含这些化合物的制药组合物以及使用这些化合物和组合物预防或治疗CGRP参与的这些疾病的用途。