tert-butyl 4-[2-(2-methoxy-2-oxoethyl)phenyl]-3,6-dihydro-2H-pyridine-1-carboxylate | 951774-85-9

• 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
• 英文名称: tert-butyl 4-[2-(2-methoxy-2-oxoethyl)phenyl]-3,6-dihydro-2H-pyridine-1-carboxylate
• CAS: 951774-85-9
• 化学式: C₁₉H₂₅NO₄
• 分子量: 331.412
• InChiKey: WCJOMMAMJVNFSW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  55.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl 4-[2-(2-methoxy-2-oxoethyl)phenyl]-3,6-dihydro-2H-pyridine-1-carboxylate 在 platinum(IV) oxide 氢气 作用下， 以 乙醇 、 溶剂黄146 为溶剂， 反应 2.0h， 生成 Tert-butyl 4-[2-(2-methoxy-2-oxoethyl)phenyl]piperidine-1-carboxylate
  参考文献：
  名称：

  Phenylpiperidine derivatives as melanocortin-4 receptor modulators

  摘要：

  本发明涉及取代苯基哌啶衍生物作为黑色素皮质素-4受体调节剂。根据结构和立体化学，本发明的化合物要么是人类黑色素皮质素-4受体（MC-4R）的选择性激动剂，要么是选择性拮抗剂。激动剂可用于治疗肥胖、糖尿病和性功能障碍等疾病，而拮抗剂可用于治疗癌症恶病质、肌肉消耗、厌食症、焦虑和抑郁等疾病。一般来说，涉及MC-4R调节的所有疾病和疾病都可以用本发明的化合物进行治疗。

  公开号：

  EP1842846A1
• 作为产物：
  描述：

  2-(2-溴苯基)乙酸甲酯 、 N-Boc-1,2,5,6-四氢吡啶-4-硼酸频哪醇酯 在 1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 tert-butyl 4-[2-(2-methoxy-2-oxoethyl)phenyl]-3,6-dihydro-2H-pyridine-1-carboxylate
  参考文献：
  名称：

  Substituted aryl or heteroarylpiperidine derivatives as melanocortin-4 receptor modulators

  摘要：

  本发明涉及结构式(I)的取代芳基或杂芳基哌啶衍生物，作为黑色素皮质素-4受体调节剂。根据结构和立体化学，本发明的化合物可以是人类黑色素皮质素-4受体(MC-4R)的选择性激动剂或选择性拮抗剂。激动剂可用于治疗肥胖、糖尿病和性功能障碍等疾病，而拮抗剂可用于治疗癌症恶病质、肌肉消耗、厌食症、焦虑和抑郁等疾病。一般来说，所有涉及MC-4R调节的疾病和疾病都可以用本发明的化合物进行治疗。

  公开号：

  EP2020405A1

文献信息

• Phenylpiperidine derivatives as melanocortin-4 receptor modulators
  申请人：Santhera Pharmaceuticals (Schweiz) AG

  公开号：EP1842846A1

  公开（公告）日：2007-10-10

  The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.

  本发明涉及取代苯基哌啶衍生物作为黑色素皮质素-4受体调节剂。根据结构和立体化学，本发明的化合物要么是人类黑色素皮质素-4受体（MC-4R）的选择性激动剂，要么是选择性拮抗剂。激动剂可用于治疗肥胖、糖尿病和性功能障碍等疾病，而拮抗剂可用于治疗癌症恶病质、肌肉消耗、厌食症、焦虑和抑郁等疾病。一般来说，涉及MC-4R调节的所有疾病和疾病都可以用本发明的化合物进行治疗。
• SUBSTITUTED PHENYLPIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS
  申请人：Santhera Pharmaceuticals (Schweiz) AG

  公开号：EP2004604B1

  公开（公告）日：2010-12-01
• Substituted Phenylpiperidine Derivatives As Melanocortin-4 Receptor Modulators
  申请人：Soeberdt Michael

  公开号：US20110086836A1

  公开（公告）日：2011-04-14

  The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
• [EN] SUBSTITUTED PHENYLPIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS DE PHÉNYLPIPÉRIDINE SUBSTITUÉS EN TANT QUE MODULATEURS DU RÉCEPTEUR DE LA MÉLANOCORTINE-4
  申请人：SANTHERA PHARMACEUTICALS CH

  公开号：WO2007115798A1

  公开（公告）日：2007-10-18

  [EN] The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
  [FR] La présente invention concerne des dérivés de phénylpipéridine substitués en tant que modulateurs des récepteurs de la mélanocortine-4. En fonction de la structure et de la stéréochimie, les composés de l'invention sont soit des agonistes sélectifs, soit des antagonistes sélectifs du récepteur humain de la mélanocortine-4 (MC-4R). Les agonistes peuvent être utilisés pour le traitement de troubles et de maladies tels que l'obésité, le diabète et une dysfonction sexuelle, alors que les antagonistes sont utiles pour le traitement de troubles et de maladies tels que le cancer, l'émaciation, l'atrophie musculaire, l'anorexie, l'anxiété et la dépression. Généralement, toutes les maladies et tous les troubles associés à la régulation du MC-4R peuvent être traités avec les composés de l'invention.
• [EN] SUBSTITUTED ARYL OR HETEROARYLPIPERDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS SUBSTITUÉS D'ARYL OU HÉTÉROARYLPIPÉRIDINE COMME MODULATEURS DU RÉCEPTEUR 4 DE LA MÉLANOCORTINE
  申请人：SANTHERA PHARMACEUTICALS CH

  公开号：WO2009015867A1

  公开（公告）日：2009-02-05

  The present invention relates to substituted aryl or heteroarylpiperidine derivatives of structure (I) as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC- 4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, amyotrophic lateral sclerosis (ALS), anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.