2-溴甲基-3-氯-5-三氟甲基-吡啶 | 1227502-50-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 2-溴甲基-3-氯-5-三氟甲基-吡啶
• 英文名称: 3-chloro-5-trifluoromethyl-2-bromomethylpyridine
• 英文别名: 2-Bromomethyl-3-chloro-5-trifluoromethyl-pyridine；2-(Bromomethyl)-3-chloro-5-(trifluoromethyl)pyridine
• CAS: 1227502-50-2
• 化学式: C₇H₄BrClF₃N
• 分子量: 274.468
• InChiKey: WPALGCBMYXXOSU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  12.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-溴甲基-3-氯-5-三氟甲基-吡啶 生成 2-[Bis-(2-hydroxy-ethyl)-amino]-5-[1-(3-chloro-5-trifluoromethyl-pyridin-2-ylmethyl)-1H-indazol-5-ylmethylene]-thiazol-4-one
  参考文献：
  名称：

  AMINOTHIAZOLONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS

  摘要：

  本发明涉及式（I）的化合物，制备这些化合物的方法，组合物，中间体及其衍生物，并用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童关节炎，银屑病性关节炎，反应性关节炎），骨相关疾病（包括与骨形成有关的疾病），乳腺癌（包括对抗雌激素治疗无效的癌症），心血管疾病，软骨相关疾病（如软骨损伤/丧失，软骨退化，以及与软骨形成有关的疾病），软骨发育不良，软骨肉瘤，慢性背部受伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺疾病，糖尿病，能量稳态失调疾病，痛风，假性痛风，脂质代谢紊乱，代谢综合征，多发性骨髓瘤，肥胖，骨关节炎，进行性骨折性骨转移，软骨软化症，骨质疏松症，帕吉特病，牙周疾病，多肌痛风，Reiter综合征，重复性应力损伤，高血糖，血糖水平升高和胰岛素抵抗等症状的方法。

  公开号：

  US20110200586A1
• 作为产物：
  描述：

  [3-氯-5-(三氟甲基)吡啶-2-基]甲醇 在 三溴化磷 作用下， 以 二氯甲烷 为溶剂， 反应 4.5h， 以89.2%的产率得到2-溴甲基-3-氯-5-三氟甲基-吡啶
  参考文献：
  名称：

  2-氨甲基-3-氯-5-三氟甲基吡啶盐酸盐的制备方法

  摘要：

  本发明公开一种2‑氨甲基‑3‑氯‑5‑三氟甲基吡啶盐酸盐的制备方法，属于农有机化学合成领域，按照下述步骤制备：以3‑氯‑5‑三氟甲基‑2‑吡啶甲醇为原料，与三溴化磷反应得中间体3‑氯‑5‑三氟甲基‑2‑溴甲基吡啶，然后依次与六次甲基四胺和浓盐酸反应得2‑氨甲基‑3‑氯‑5‑三氟甲基吡啶盐酸盐；本发明的制备方法具有以下有益效果：原料易于购买，有机溶剂和碱可以回收，收率较高，产品质量好，是适合制备2‑氨甲基‑3‑氯‑5‑三氟甲基吡啶盐酸盐的方法。

  公开号：

  CN107216284A

文献信息

• CYCLOPROPYL MODULATORS OF P2Y12 RECEPTOR
  申请人：Rao Tadimeti

  公开号：US20120301458A1

  公开（公告）日：2012-11-29

  The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof

  本发明涉及P2Y12受体活性的新环丙基调节剂，其制药组合物以及使用方法。
• Aminothiazolones as estrogen related receptor-alpha modulators
  申请人：Bignan Gilles

  公开号：US08426604B2

  公开（公告）日：2013-04-23

  The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

  本发明涉及公式（I）的化合物，制备这些化合物的方法，组成物，中间体和衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童关节炎，银屑病性关节炎，反应性关节炎），骨相关疾病（包括与骨形成有关的疾病），乳腺癌（包括对抗雌激素治疗无效的乳腺癌），心血管疾病，软骨相关疾病（如软骨损伤/丧失，软骨退化和与软骨形成有关的疾病），软骨发育不良，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺疾病，糖尿病，能量稳态失调疾病，痛风，假性痛风，脂质代谢紊乱，代谢综合征，多发性骨髓瘤，肥胖症，骨关节炎，骨发育不全，骨转移性溶骨病，软骨软化症，骨质疏松症，帕吉特病，牙周病，多肌病性风湿病，Reiter综合症，重复性应力损伤，高血糖，血糖水平升高和胰岛素抵抗等疾病。
• US8426604B2
  申请人：——

  公开号：US8426604B2

  公开（公告）日：2013-04-23
• [EN] AMINOTHIAZOLONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS<br/>[FR] AMINOTHIAZOLONES EN TANT QUE MODULATEURS DE RÉCEPTEUR ALPHA ASSOCIÉ AUX OESTROGÈNES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2011103130A1

  公开（公告）日：2011-08-25

  The present invention relates to compounds of Formula (I): methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone- related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
• AMINOTHIAZOLONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS
  申请人：BIGNAN Gilles

  公开号：US20110200586A1

  公开（公告）日：2011-08-18

  The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

  本发明涉及式（I）的化合物，制备这些化合物的方法，组合物，中间体及其衍生物，并用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童关节炎，银屑病性关节炎，反应性关节炎），骨相关疾病（包括与骨形成有关的疾病），乳腺癌（包括对抗雌激素治疗无效的癌症），心血管疾病，软骨相关疾病（如软骨损伤/丧失，软骨退化，以及与软骨形成有关的疾病），软骨发育不良，软骨肉瘤，慢性背部受伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺疾病，糖尿病，能量稳态失调疾病，痛风，假性痛风，脂质代谢紊乱，代谢综合征，多发性骨髓瘤，肥胖，骨关节炎，进行性骨折性骨转移，软骨软化症，骨质疏松症，帕吉特病，牙周疾病，多肌痛风，Reiter综合征，重复性应力损伤，高血糖，血糖水平升高和胰岛素抵抗等症状的方法。