(R)-tert-butyl (1-hydrazinyl-2-methyl-1-oxo-3-phenylpropan-2-yl)carbamate | 868286-25-3

• 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: (R)-tert-butyl (1-hydrazinyl-2-methyl-1-oxo-3-phenylpropan-2-yl)carbamate
• 英文别名: (R)-N-(fert-butoxycarbonyl)-α-methylphenylalaninehydrazide；N-(tert-butoxycarbonyl)-α-methyl-D-phenylalanine hydrazide；(R)-N-(tert-butoxycarbonyl)-α-methylphenylalanmehydrazide；R-N-(tert-butoxycarbonyl)-α-methylphenylalaninhydrazamide；(R)-2-tert-butoxycarbonylamino-2-benzylpropanehydrazide；tert-butyl N-[(2R)-1-hydrazinyl-2-methyl-1-oxo-3-phenylpropan-2-yl]carbamate
• CAS: 868286-25-3
• 化学式: C₁₅H₂₃N₃O₃
• 分子量: 293.366
• InChiKey: NISOMEWSXGQXJW-OAHLLOKOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  93.4
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R)-tert-butyl (1-hydrazinyl-2-methyl-1-oxo-3-phenylpropan-2-yl)carbamate 在 二(三叔丁基膦)钯 potassium phosphate 、 N-羟基-7-氮杂苯并三氮唑 、 methoxycarbonylsulfamoyl-triethylammonium hydroxide 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 作用下， 以 DMF (N,N-dimethyl-formamide) 、 1,2-二氯乙烷 为溶剂， 反应 29.17h， 生成 tert-butyl (1R)-1R-methyl-1-(5-{2-({(1S)-1-[(1S,2S)-2-methylcyclopropyl]ethyl}amino)-6-[methyl(methylsulfonyl)amino]pyridin-4-yl}-1,3,4-oxadiazol-2-yl)-2-phenylethylcarbamate
  参考文献：
  名称：

  [EN] 2, 4, 6-SUBSTITUTED PYRIDYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
  [FR] COMPOSES DERIVES DE PYRIDYLE SUBSTITUES AUX POSITIONS 2, 4, 6 UTILES COMME INHIBITEURS DE LA BETA-SECRETASE DANS LE TRAITEMENT DE LA MALADIE D'ALZHEIMER

  摘要：

  本发明涉及2,4,6-取代吡啶衍生物化合物，这些化合物是β-分泌酶的抑制剂，可用于治疗涉及β-分泌酶的疾病，如阿尔茨海默病。该发明还涉及包含这些化合物的药物组合物以及在治疗涉及β-分泌酶的疾病中使用这些化合物和组合物。

  公开号：

  WO2005103043A1
• 作为产物：
  描述：

  α-甲基-D-苯丙氨酸 在 sodium hydroxide 、 水 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 肼 作用下， 以 1,4-二氧六环 、 乙腈 为溶剂， 反应 15.0h， 生成 (R)-tert-butyl (1-hydrazinyl-2-methyl-1-oxo-3-phenylpropan-2-yl)carbamate
  参考文献：
  名称：

  [EN] 2, 4, 6-SUBSTITUTED PYRIDYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
  [FR] COMPOSES DERIVES DE PYRIDYLE SUBSTITUES AUX POSITIONS 2, 4, 6 UTILES COMME INHIBITEURS DE LA BETA-SECRETASE DANS LE TRAITEMENT DE LA MALADIE D'ALZHEIMER

  摘要：

  本发明涉及2,4,6-取代吡啶衍生物化合物，这些化合物是β-分泌酶的抑制剂，可用于治疗涉及β-分泌酶的疾病，如阿尔茨海默病。该发明还涉及包含这些化合物的药物组合物以及在治疗涉及β-分泌酶的疾病中使用这些化合物和组合物。

  公开号：

  WO2005103043A1

文献信息

• [EN] OXADIAZOLE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF<br/>[FR] COMPOSÉS OXADIAZOLE QUI INHIBENT L'ACTIVITÉ DE LA BÊTA-SECRÉTASE, ET LEURS PROCÉDÉS D'UTILISATION
  申请人：COMENTIS INC

  公开号：WO2012054510A1

  公开（公告）日：2012-04-26

  The invention provides novel beta-secretase inhibitors and methods for their including methods of treating Alzheimer's disease.

  这项发明提供了新型β-分泌酶抑制剂以及它们的方法，包括治疗阿尔茨海默病的方法。
• [EN] 1,3,5-SUBSTITUTED PHENYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE<br/>[FR] DERIVES DE PHENYLE 1,3,5-SUBSTITUES UTILES COMME INHIBITEURS DE LA BETA-SECRETASE POUR LE TRAITEMENT DE LA MALADIE D'ALZHEIMER
  申请人：MERCK & CO INC

  公开号：WO2005103020A1

  公开（公告）日：2005-11-03

  The present invention is directed to 1,3,5-phenyl substituted derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及1,3,5-苯基取代衍生物化合物，这些化合物是β-分泌酶的抑制剂，可用于治疗β-分泌酶参与的疾病，例如阿尔茨海默病。该发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在治疗β-分泌酶参与疾病中的用途。
• Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
  申请人：Nanternet Philippe G.

  公开号：US20090182021A1

  公开（公告）日：2009-07-16

  The present invention is directed to tricyclic compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及三环化合物，它们是β-分泌酶的抑制剂，并且在治疗β-分泌酶参与的疾病，如阿尔茨海默病中有用。该发明还涉及包含这些化合物的药物组合物，以及在治疗β-分泌酶参与的这类疾病中使用这些化合物和组合物。
• 1,3,5-Substituted Phenyl Derivative Compounds Useful as Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
  申请人：Barrow C. James

  公开号：US20070244119A1

  公开（公告）日：2007-10-18

  The present invention is directed to 1,3,5-phenyl substituted derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及一类1,3,5-苯基取代衍生物化合物，它们是β-分泌酶酶的抑制剂，可用于治疗β-分泌酶酶参与的疾病，如阿尔茨海默病。本发明还涉及包含这些化合物的制药组合物，以及这些化合物和组合物在治疗β-分泌酶酶参与的疾病中的用途。
• Aminomethyl Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
  申请人：Coburn Craig A.

  公开号：US20080153846A1

  公开（公告）日：2008-06-26

  The present invention is directed to aminomethyl compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及氨甲基化合物，它们是β-分泌酶酶的抑制剂，并且在β-分泌酶酶参与的疾病的治疗中非常有用，例如阿尔茨海默病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在β-分泌酶酶参与的这些疾病的治疗中的用途。