tert-butyl 6-bromo-4-hydroxyspiro[chromane-2,4’-piperidine]-1‘-carboxylate | 945722-85-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: tert-butyl 6-bromo-4-hydroxyspiro[chromane-2,4’-piperidine]-1‘-carboxylate
• 英文别名: tert-butyl 6-bromo-4-hydroxyspiro[chromane-2,4’-piperidine]-1’-carboxylate；tert-butyl 6-bromo-4-hydroxy-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxylate；Tert-butyl 6-bromo-4-hydroxyspiro[chromane-2,4'-piperidine]-1'-carboxylate；tert-butyl 6-bromo-4-hydroxyspiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxylate
• CAS: 945722-85-0
• 化学式: C₁₈H₂₄BrNO₄
• 分子量: 398.297
• InChiKey: CFVANMVMPHRECH-UHFFFAOYSA-N

物化性质

• 沸点：
  487.3±45.0 °C(Predicted)
• 密度：
  1.44±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  59
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl 6-bromo-4-hydroxyspiro[chromane-2,4’-piperidine]-1‘-carboxylate 在 三乙基硅烷 、 三氟乙酸 作用下， 反应 7.5h， 以90%的产率得到6-溴螺[苯并二氢吡喃-2,4-哌啶]
  参考文献：
  名称：

  WO2007/88462

  摘要：

  公开号：
• 作为产物：
  描述：

  N-叔丁氧羰基-4-哌啶酮 在 四氢吡咯 、 sodium tetrahydroborate 作用下， 以 甲醇 、 乙醇 为溶剂， 反应 4.0h， 生成 tert-butyl 6-bromo-4-hydroxyspiro[chromane-2,4’-piperidine]-1‘-carboxylate
  参考文献：
  名称：

  螺环化合物、其制备方法、中间体、药物组合物 和应用

  摘要：

  本发明公开了一种如式I所示的螺环化合物、其药学上可接受的盐、水合物、溶剂合物、其光学异构体或其前药，其制备方法、中间体、药物组合物及其应用。本发明的螺环化合物具有作为蛋白激酶抑制剂、包括作为c‑Met等酪氨酸激酶抑制剂的活性，并可用于治疗因这些激酶的异常活性引起的疾病，例如癌症等，或者用于制备治疗这些疾病的药物。

  公开号：

  CN103304571B

文献信息

• TRICYCLIC SPIROCYCLE DERIVATIVES AND METHODS OF USE
  申请人：McCormick Kevin D.

  公开号：US20110166124A1

  公开（公告）日：2011-07-07

  The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.

  本发明涉及新型三环螺环衍生物，包括该三环螺环衍生物的药物组合物，以及利用这些化合物治疗或预防过敏、过敏引起的气道反应、充血、心血管疾病、炎症性疾病、消化系统紊乱、神经系统紊乱、代谢紊乱、肥胖或与肥胖相关的疾病、糖尿病、糖尿病并发症、糖耐量受损或空腹血糖异常。
• [EN] SPIROPIPERIDINE DERIVATIVES<br/>[FR] DÉRIVÉS DE SPIROPIPÉRIDINE
  申请人：CEPHALON INC

  公开号：WO2018112204A1

  公开（公告）日：2018-06-21

  Described herein are spiropiperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described spiropiperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described spiropiperidine compounds and synthetic intermediates that are useful in those syntheses.

  本文所述的是根据式I的螺哌啶化合物，它们已显示出作为脂肪酸合成酶抑制剂的活性。本文还描述了含有所述螺哌啶化合物的药物组合物，以及通过施用本文所述的一种或多种化合物或药物制剂来治疗由脂肪酸合成酶介导的疾病的方法。本文还描述了合成所述化合物的方法，包括所述螺哌啶化合物及其在那些合成中有用的合成中间体。
• [EN] 3-SPIRO-7-HYDROXAMIC ACID TETRALINS AS HDAC INHIBITORS<br/>[FR] TÉTRALINES DE 3-SPIRO-7-ACIDE HYDROXAMIQUE EN TANT QU'INHIBITEURS DE HDAC
  申请人：FORMA THERAPEUTICS INC

  公开号：WO2016168660A1

  公开（公告）日：2016-10-20

  The present invention is directed to compounds of Formulae I and II which are inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.

  本发明涉及式I和式II化合物，它们是组蛋白去乙酰化酶（HDACs）的抑制剂，如HDAC6，并且它们在治疗细胞增殖性疾病（如癌症）、神经系统疾病（如神经退行性疾病或神经发育疾病）、炎症性或自身免疫疾病、感染、代谢性疾病、血液疾病或心血管疾病中的应用。
• Spiropiperidine derivatives
  申请人：89BIO LTD

  公开号：US11046707B2

  公开（公告）日：2021-06-29

  Described herein are spiropiperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described spiropiperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described spiropiperidine compounds and synthetic intermediates that are useful in those syntheses.

  本文描述了根据式 I 的螺环哌啶化合物，这些化合物作为脂肪酸合成酶抑制剂已被证明具有活性。本文还描述了含有所述螺哌啶化合物的药物组合物，以及通过施用一种或多种本文所述化合物或药物制剂治疗由脂肪酸合成酶介导的疾病的方法。本文还描述了合成所述化合物的方法，包括所述螺哌啶化合物和在这些合成中有用的合成中间体。
• 3-SPIRO-7-HYDROXAMIC ACID TETRALINS AS HDAC INHIBITORS
  申请人：Forma Therapeutics, Inc.

  公开号：US20160304462A1

  公开（公告）日：2016-10-20

  The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.