N-Cbz-3(S)-氟吡咯烷 | 136725-52-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-Cbz-3(S)-氟吡咯烷
• 中文别名: 3(S)-氟吡咯烷-1-甲酸苄酯；N-CBZ-3-(S)-氟吡咯烷
• 英文名称: (S)-N-CBz-3-fluoropyrrolidine
• 英文别名: benzyl (3S)-3-fluoropyrrolidine-1-carboxylate；(3S)-3-Fluoro-pyrrolidine-1-carboxylic Acid Benzyl Ester
• CAS: 136725-52-5
• 化学式: C₁₂H₁₄FNO₂
• 分子量: 223.247
• InChiKey: DGQYMNWQXVFIBE-NSHDSACASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-Cbz-3(S)-氟吡咯烷 在 palladium 10% on activated carbon 氢气 、 盐酸 作用下， 以 乙醇 、 乙醚 为溶剂， 反应 4.5h， 生成 (S)-3-fluoropyrrolidine hydrochloride
  参考文献：
  名称：

  Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)

  摘要：

  本发明涉及一种式(I)的化合物，它们抑制二肽基肽酶IV（DPP-IV），并且可用于预防或治疗糖尿病，特别是II型糖尿病，以及高血糖、X综合征、高胰岛素血症、肥胖、动脉粥样硬化和各种免疫调节性疾病。

  公开号：

  US20050209249A1
• 作为产物：
  描述：

  N-CBZ-3-(R)-羟基吡咯烷 在 二乙胺基三氟化硫 作用下， 以 二氯甲烷 为溶剂， 生成 N-Cbz-3(S)-氟吡咯烷
  参考文献：
  名称：

  [EN] 1,2,4-OXADIAZOLE DERIVATIVES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
  [FR] DERIVES DE 1,2,4-OXADIAZOLE EN TANT QU'INHIBITEURS DE LA DIPEPTIDYLPEPTIDASE-IV DANS LE TRAITEMENT OU LA PREVENTION DE DIABETES

  摘要：

  本发明涉及一种新颖的1,2,4-噁二唑衍生物，这些衍生物是二肽基肽酶-IV酶（'DP-IV抑制剂'）的抑制剂，并且在治疗或预防涉及二肽基肽酶-IV酶的疾病方面具有用处，例如糖尿病，特别是2型糖尿病。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预防或治疗涉及二肽基肽酶-IV酶的疾病方面的用途。

  公开号：

  WO2005108382A1

文献信息

• Methods for Production of Optically Active Fluoropyrrolidine Derivatives
  申请人：Umemoto Teruo

  公开号：US20100174096A1

  公开（公告）日：2010-07-08

  Useful industrial methods for producing optically active fluoropyrrolidine derivatives as useful fluorinated intermediates are disclosed.

  揭示了用于生产光学活性氟吡咯烷衍生物的有用工业方法，作为有用的氟化中间体。
• [EN] PHENYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES<br/>[FR] DERIVES DE PHENYLALANINE UTILISES COMME INHIBITEURS DE LA DIPEPTIDYL PEPTIDASE DANS LE TRAITEMENT OU LA PREVENTION DU DIABETE
  申请人：MERCK & CO INC

  公开号：WO2004043940A1

  公开（公告）日：2004-05-27

  The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

  本发明涉及苯丙氨酸衍生物，这些衍生物是二肽基肽酶-IV酶（'DP-IV抑制剂'）的抑制剂，并且在治疗或预防涉及二肽基肽酶-IV酶的疾病中具有用处，如糖尿病，特别是2型糖尿病。该发明还涉及包含这些化合物的药物组合物以及在预防或治疗涉及二肽基肽酶-IV酶的这类疾病中使用这些化合物和组合物。
• [EN] CYCLOHEXYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES<br/>[FR] DERIVES DE LA CYCLOHEXYLALANINE UTILISES COMME INHIBITEURS DE LA DIPEPTIDYL PEPTIDASE-IV POUR LE TRAITEMENT OU LA PREVENTION DES DIABETES
  申请人：MERCK & CO INC

  公开号：WO2005116029A1

  公开（公告）日：2005-12-08

  The present invention is directed to novel cyclohexylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

  本发明涉及新颖的环己基丙氨酸衍生物，这些衍生物是二肽基肽酶-IV酶（'DP-IV抑制剂'）的抑制剂，并且在治疗或预防涉及二肽基肽酶-IV酶的疾病中具有用处，如糖尿病，特别是2型糖尿病。该发明还涉及包含这些化合物的药物组合物，以及在预防或治疗涉及二肽基肽酶-IV酶的这类疾病中使用这些化合物和组合物。
• Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
  申请人：Duffy L. Joseph

  公开号：US20060111336A1

  公开（公告）日：2006-05-25

  The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

  本发明涉及苯丙氨酸衍生物，它们是二肽基肽酶-IV酶（“DP-IV酶”）的抑制剂，可用于治疗或预防DP-IV酶参与的疾病，例如糖尿病，特别是2型糖尿病。本发明还涉及包含这些化合物的制药组合物，以及使用这些化合物和组合物预防或治疗DP-IV酶参与的这些疾病。
• N-acyl-substituted azacyclic compounds, processes for their preparation,
  申请人：Dr. Lo Zembeletti S.p.A.

  公开号：US05322848A1

  公开（公告）日：1994-06-21

  A compound, or solvate or salt thereof, of formula ##STR1## R.sub.1 is hydrogen, halogen, or C.sub.1-6 alkyl; R.sub.2 and R.sub.3 are hydrogen or C.sub.1-6 alkyl; R.sub.5 together with R.sub.4 forms a --(CH).sub.2).sub.2 -- group optionally substituted by one or two C.sub.1-6 alkyl; W is halogen or when A is gem-dimethyl substituted piperidine, is OH; a is 1 or 2, useful in the treatment of pain.

  化合物的分子式为##STR1## 其中R.sub.1为氢、卤素或C.sub.1-6烷基；R.sub.2和R.sub.3为氢或C.sub.1-6烷基；R.sub.5与R.sub.4一起形成一个-（CH）.sub.2）.sub.2-基团，可选地被一个或两个C.sub.1-6烷基取代；W为卤素或当A为双甲基取代的哌啶时，为OH；a为1或2，可用于治疗疼痛。