3-(2 (R)-cyclopentylmethyl-3(S)-hydroxyl-5-phenyl-1-oxopentyl)-4(R)-(phenylmethyl)-2-oxazolidinone | 330841-07-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: 3-(2 (R)-cyclopentylmethyl-3(S)-hydroxyl-5-phenyl-1-oxopentyl)-4(R)-(phenylmethyl)-2-oxazolidinone
• 英文别名: (4R)-4-benzyl-3-[(2R,3S)-2-(cyclopentylmethyl)-3-hydroxy-5-phenylpentanoyl]-1,3-oxazolidin-2-one
• CAS: 330841-07-1
• 化学式: C₂₇H₃₃NO₄
• 分子量: 435.563
• InChiKey: LOLAZXMQEWBYLP-SDHSZQHLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  32
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-(2 (R)-cyclopentylmethyl-3(S)-hydroxyl-5-phenyl-1-oxopentyl)-4(R)-(phenylmethyl)-2-oxazolidinone 在 lithium hydroxide 、 双氧水 、 sodium sulfite 作用下， 以 四氢呋喃 、 水 、 乙酸乙酯 为溶剂， 以230 mg (81%)的产率得到2(R)-Cyclopentylmethyl-3(S)-hydroxyl-5-phenylpentanoic Acid
  参考文献：
  名称：

  Hydroxyalkanoylaminolactams and related structures as inhibitors of a &bgr; protein production

  摘要：

  本发明涉及具有以下化学式(I)的新型内酰胺，以及它们的药物组合物和使用方法。这些新型化合物抑制淀粉样前体蛋白的加工，更具体地说，抑制Aβ-肽的产生，从而防止淀粉样蛋白在神经系统中的沉积形成。更具体地说，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，如阿尔茨海默病和唐氏综合征。

  公开号：

  US06503902B2
• 作为产物：
  描述：

  (R)-4-苄基-3-(3-环戊基丙酰基)-噁唑啉-2-酮 、 di-n-butylboron trifluoromethanesulphonate 、 三乙胺 、 、 苯丙醛 在 氮气 、 磷酸肌酸 、 甲醇 、 双氧水 、 three 、 乙醚 、 碳酸氢钠 、 Brine 、 magnesium sulfate 、 ethyl acetate n-hexane 作用下， 以 二氯甲烷 为溶剂， 反应 2.08h， 以provided 1.11 g (56%) of aldol 3 as a colorless oil的产率得到3-(2 (R)-cyclopentylmethyl-3(S)-hydroxyl-5-phenyl-1-oxopentyl)-4(R)-(phenylmethyl)-2-oxazolidinone
  参考文献：
  名称：

  Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production

  摘要：

  本发明涉及具有以下式(I)的新型内酰胺、它们的制药组合物以及它们的使用方法。这些新型化合物抑制淀粉样前体蛋白的加工，更具体地抑制Aβ-肽的产生，从而防止神经元淀粉样蛋白的沉积形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，如阿尔茨海默病和唐氏综合征。

  公开号：

  US06960576B2

文献信息

• Hydroxyalkanoylaminolactams and related structures as inhibitors of a beta protein production
  申请人：——

  公开号：US20020052360A1

  公开（公告）日：2002-05-02

  This invention relates to novel lactams having the formula (I): 1 to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有公式(I)的新颖内酰胺：1及其药物组合物及其使用方法。这些新颖化合物抑制淀粉样前体蛋白的加工，更具体地说，抑制Aβ-肽的产生，从而防止神经系统中淀粉样蛋白沉积的形成。更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，如阿尔茨海默病和唐氏综合症。
• Hydroxyalkanoylaminolactams and related structures as inhibitors of a &bgr; protein production
  申请人：Bristol-Myers Squibb Pharma Company

  公开号：US06503902B2

  公开（公告）日：2003-01-07

  This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有以下化学式(I)的新型内酰胺，以及它们的药物组合物和使用方法。这些新型化合物抑制淀粉样前体蛋白的加工，更具体地说，抑制Aβ-肽的产生，从而防止淀粉样蛋白在神经系统中的沉积形成。更具体地说，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，如阿尔茨海默病和唐氏综合征。
• Hydroxyalkanoylaminolactams and related structures as inhibitors of A beta protein production
  申请人：Olson E. Richard

  公开号：US20050113363A1

  公开（公告）日：2005-05-26

  This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有公式(I)的新型内酰胺，它们的制药组合物以及它们的使用方法。这些新型化合物抑制淀粉样前体蛋白的加工，更具体地抑制Aβ肽的产生，从而防止神经淀粉样蛋白沉积物的形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，例如阿尔茨海默病和唐氏综合症。
• Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
  申请人：Bristol-Myers Squibb Pharma Company

  公开号：US07112583B2

  公开（公告）日：2006-09-26

  This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有以下式子(I)的新型内酰胺，其药物组成和使用方法。这些新化合物抑制淀粉样前体蛋白的加工，更具体地抑制Aβ-肽的产生，从而防止神经元沉积淀粉样蛋白的形成。更具体地，本发明涉及与β-淀粉样蛋白产生有关的神经系统疾病的治疗，如阿尔茨海默病和唐氏综合征。
• Hydroxyalkanoylaminolactams and related structures as inhibitors of Alphabeta protein production
  申请人：Olson E. Richard

  公开号：US20070027132A1

  公开（公告）日：2007-02-01

  This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

  本发明涉及具有公式（I）的新型内酰胺，其制药组合物以及使用方法。这些新型化合物抑制淀粉样前体蛋白的加工，更具体地抑制Aβ-肽的产生，从而防止神经沉积物的淀粉样蛋白形成。更具体地，本发明涉及与β-淀粉样蛋白产生相关的神经系统疾病的治疗，例如阿尔茨海默病和唐氏综合症。