4-(2-fluoro-3-(trifluoromethyl)phenyl)thiazol-2-amine | 444143-17-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-(2-fluoro-3-(trifluoromethyl)phenyl)thiazol-2-amine
• 英文别名: 4-[2-fluoro-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-amine；4-(2-fluoro-3-trifluoromethyl-phenyl)-1,3-thiazol-2-amine；4-(2-fluoro-3-trifluoromethyl-phenyl)-thiazol-2-ylamine
• CAS: 444143-17-3
• 化学式: C₁₀H₆F₄N₂S
• mdl: MFCD06739841
• 分子量: 262.231
• InChiKey: QTFIQKQWACKFHA-UHFFFAOYSA-N

物化性质

• 沸点：
  359.1±42.0 °C(Predicted)
• 密度：
  1.478±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  67.2
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  4-(2-fluoro-3-(trifluoromethyl)phenyl)thiazol-2-amine 、 4-碘苯甲酰氯 生成 N-(4-(2-fluoro-3-(trifluoromethyl)phenyl)thiazol-2-yl)-4-iodobenzene
  参考文献：
  名称：

  Pyrimidine benzamide-based thrombopoietin receptor agonists

  摘要：

  A series of pyrimidine benzamide-based thrombopoietin receptor agonists is described. The lead molecule contains a 2-amino-5-unsubstituted thiazole, a group that has been associated with idiosyncratic toxicity. The potential for metabolic oxidation at C-5 of the thiazole, the likely source of toxic metabolites, was removed by substitution at C-5 or by replacing the thiazole with a thiadiazole. Potency in the series was improved by modifying the substituents on the pyrimidine and/or on the thiazole or thiadiazole pendant aryl ring. In vivo examination revealed that compounds from the series are not highly bioavailable. This is attributed to low solubility and poor permeability. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.07.038
• 作为产物：
  描述：

  2-氟-3-(三氟甲基)苯乙酮 在 磺酰氯 、 硫脲 作用下， 以 乙醇 为溶剂， 反应 26.0h， 以74%的产率得到4-(2-fluoro-3-(trifluoromethyl)phenyl)thiazol-2-amine
  参考文献：
  名称：

  WO2007/4038

  摘要：

  公开号：

文献信息

• [EN] FUSED PYRIMIDINE-DIONE DERIVATIVES AS TRPA1 MODULATORS<br/>[FR] DÉRIVÉS DE PYRIMIDINEDIONES FUSIONNÉS UTILISÉS COMME MODULATEURS DES RÉCEPTEURS TRPA1
  申请人：GLENMARK PHARMACEUTICALS SA

  公开号：WO2010109287A1

  公开（公告）日：2010-09-30

  The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPAl (Transient Receptor Potential subfamily A, member 1). This invention also provides processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPAl. Formula (I)

  本发明描述的是一类新颖的杂合吡啶二酮衍生物，其化学公式为（I），这些衍生物是TRPA（瞬时受体电位亚家族A）的调节剂。特别是，本文所述的化合物对于治疗或预防由TRPA1（瞬时受体电位亚家族A成员1）调控的疾病、状况和/或失调是有用的。本发明还提供了制备所述化合物、它们合成中使用的中间体、药物组合物以及治疗或预防由TRPA1调控的疾病、状况和/或失调的方法。公式（I）
• Thrombopoietin Receptor Agonists
  申请人：Reiter Lawrence A.

  公开号：US20080076771A1

  公开（公告）日：2008-03-27

  A compound of the formula (I) useful as promoters of thrombopoiesis and megakaryocytopoiesis, wherein A, B, D, E, W, X, Y, Z, R 1 and R 2 are defined as above.

  一种化合物，其化学式为（I），可用作促进血小板生成和巨核细胞生成的促进剂，其中A、B、D、E、W、X、Y、Z、R1和R2如上所定义。
• [EN] AMIDES OF HETEROCYCLIC COMPOUNDS AS TRPA1 INHIBITORS<br/>[FR] AMIDES DE COMPOSÉS HÉTÉROCYCLIQUES À TITRE D'INHIBITEURS DE TRPA1
  申请人：GLENMARK PHARMACEUTICALS SA

  公开号：WO2011114184A1

  公开（公告）日：2011-09-22

  Amides of heterocyclic compounds as Transient Receptor Potential subfamily A (TRPA) modulators are provided In particular, compounds described herein are useful for treating or preventing diseases, conditions and/ or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1) Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. (I).

  提供了杂环化合物的酰胺作为瞬时受体电位亚家族A（TRPA）调节剂。具体来说，本文描述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚家族A，成员1）调节的疾病、症状和/或疾病。本文还提供了制备本文描述的化合物的方法、其合成中使用的中间体、药物组合物以及治疗或预防由TRPA1调节的疾病、症状和/或疾病的方法。
• [EN] PYRIMIDINEDIONE-FUSED HETEROCYCLIC COMPOUNDS AS TRPA1 MODULATORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES FUSIONNÉS À UNE PYRIMIDINE DIONE EN TANT QUE MODULATEURS DE TRPA1
  申请人：GLENMARK PHARMACEUTICALS SA

  公开号：WO2010125469A1

  公开（公告）日：2010-11-04

  The present invention is related to novel pyrimidinedione-fused heterocyclic compounds as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

  本发明涉及作为TRPA（瞬时受体电位亚家族A）调节剂的新型嘧啶二酮并环杂环化合物。具体地，本文描述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚家族A，成员1）调节的疾病、症状和/或疾病。本文还提供了用于制备本文描述的化合物的方法、用于合成的中间体、其药物组成物以及治疗或预防由TRPA1调节的疾病、症状和/或疾病的方法。
• [EN] PYRIDO[3,4-D]PYRIMIDINYL ACETAMIDE DERIVATIVES AS TRPA1 MODULATORS<br/>[FR] DÉRIVÉS DE PYRIDO[3,4-D]PYRIMIDINYL ACÉTAMIDE COMME MODULATEURS DE TRPA1
  申请人：GLENMARK PHARMACEUTICALS SA

  公开号：WO2011132017A1

  公开（公告）日：2011-10-27

  Provided are pyrido[3,4-d]pyrimidinyl acetamide derivatives as Transient Receptor Potential Ankyrin (TRPA) modulators. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Transient Receptor Potential Ankyrin 1 (TRPAl). Also provided herein are processes for preparing the compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. Formula (I).

  提供了吡啶并[3,4-d]嘧啶基乙酰胺衍生物作为瞬时受体电位蛋白鞘蛋白（TRPA）调节剂。具体来说，本文描述的化合物可用于治疗或预防由瞬时受体电位蛋白鞘蛋白1（TRPA1）调节的疾病、症状和/或疾病。本文还提供了制备所述化合物的方法、用于合成的中间体、药物组合物以及治疗或预防由TRPA1调节的疾病、症状和/或疾病的方法。公式（I）。