Methyl 3-methylsulfonyloxypyrrolidine-1-carboxylate | 428871-32-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: Methyl 3-methylsulfonyloxypyrrolidine-1-carboxylate
• CAS: 428871-32-3
• 化学式: C₇H₁₃NO₅S
• 分子量: 223.25
• InChiKey: DBWQDNGBWBMFFS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  81.3
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  Methyl 3-methylsulfonyloxypyrrolidine-1-carboxylate 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 4.08h， 生成
  参考文献：
  名称：

  Room Temperature Intramolecular Hydro-O-alkylation of Aldehydes:  sp³ C−H Functionalization via a Lewis Acid Catalyzed Tandem 1,5-Hydride Transfer/Cyclization

  摘要：

  The scope and limitations of intramolecular hydro-O-alkylation of aldehyde substrates leading to spiroketals and bicyclic ketals and aminals is reported. The direct transformation of tertiary and sterically hindered secondary sp(3) C-H bonds into C-O bonds under the action of a catalytic amount of a variety of Lewis acids is described. The mechanism of these transformations is proposed to involve a tandem hydride transfer/cyclization sequence.

  DOI：

  10.1021/ol0522283
• 作为产物：
  描述：

  甲基磺酰氯 、 甲基3-羟基-1-吡咯烷羧酸酯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 以95%的产率得到Methyl 3-methylsulfonyloxypyrrolidine-1-carboxylate
  参考文献：
  名称：

  Room Temperature Intramolecular Hydro-O-alkylation of Aldehydes:  sp³ C−H Functionalization via a Lewis Acid Catalyzed Tandem 1,5-Hydride Transfer/Cyclization

  摘要：

  The scope and limitations of intramolecular hydro-O-alkylation of aldehyde substrates leading to spiroketals and bicyclic ketals and aminals is reported. The direct transformation of tertiary and sterically hindered secondary sp(3) C-H bonds into C-O bonds under the action of a catalytic amount of a variety of Lewis acids is described. The mechanism of these transformations is proposed to involve a tandem hydride transfer/cyclization sequence.

  DOI：

  10.1021/ol0522283

文献信息

• Benzimidazole derivatives
  申请人：——

  公开号：US20040044056A1

  公开（公告）日：2004-03-04

  This invention relates to the compounds represented by a general formula [I]: 1 [in which A 1 and A 2 represent optionally fluorine-substituted methine or the like; B represents halogen, cyano, lower alkyl or the like; D represents optionally substituted heterocyclic group or the like; and G represents C 3 -C 20 aliphatic group such as alicyclic group]. These compounds inhibit nociceptin activities due to their high affinity to nociceptin receptor, and are useful as analgesic, antiobestic, corebral function improver, drugs for treatment of alzheimer's disease and dementia, remedies for schizophrenia and neurodegenerative diseases, antidepressant, remedies for diabetes insipidus, polyuria, hypotension and so on.

  本发明涉及由一般式[I]表示的化合物：1[其中，A1和A2表示选择性氟代甲基或类似物；B表示卤素，氰基，低碳烷基或类似物；D表示选择性取代的杂环基团或类似物；G表示C3-C20脂肪族基团，例如脂环族基团]。这些化合物由于对痛觉受体具有高亲和力而抑制了痛觉肽活性，并且可用作镇痛剂，抗肥胖剂，脑功能改善剂，治疗阿尔茨海默病和痴呆症的药物，治疗精神分裂症和神经退行性疾病的药物，抗抑郁剂，治疗尿崩症，多尿症，低血压等的药物。
• BENZIMIDAZOLE DERIVATIVES
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP1342717A1

  公开（公告）日：2003-09-10

  This invention relates to the compounds represented by a general formula [I]:    [in which A1 and A2 represent optionally fluorine-substituted methine or the like; B represents halogen, cyano, lower alkyl or the like; D represents optionally substituted heterocyclic group or the like; and G represents C3-C20 aliphatic group such as alicyclic group]. These compounds inhibit nociceptin activities due to their high affinity to nociceptin receptor, and are useful as analgesic, antiobestic, corebral function improver, drugs for treatment of alzheimer's disease and dementia, remedies for schizophrenia and neurodegenerative diseases, antidepressant, remedies for diabetes insipidus, polyuria, hypotension and so on.

  本发明涉及通式[I]所代表的化合物： [其中 A1 和 A2 代表任选氟取代的甲基或类似物；B 代表卤素、氰基、低级烷基或类似物；D 代表任选取代的杂环基团或类似物；G 代表 C3-C20 脂肪族基团，例如脂环族基团]。这些化合物由于与痛觉素受体的高亲和力而抑制痛觉素的活性，可用作镇痛剂、抗镇静剂、改善大脑核心功能的药物、治疗老年痴呆症和痴呆症的药物、治疗精神分裂症和神经退行性疾病的药物、抗抑郁剂、治疗糖尿病、多尿、低血压等。
• Room Temperature Hydroalkylation of Electron-Deficient Olefins:  sp³ C−H Functionalization via a Lewis Acid-Catalyzed Intramolecular Redox Event
  作者：Stefan J. Pastine、Kevin M. McQuaid、Dalibor Sames

  DOI：10.1021/ja053337f

  日期：2005.9.1

  A practical method for the intramolecular hydroalkylation of electron-deficient olefins has been developed. The direct transformation of benzylic, tertiary, and sterically hindered secondary sp3 C-H bonds into C-C bonds under the action of a catalytic amount of a variety of Lewis acids is described. The mechanism of these transformations is proposed to involve a tandem hydride transfer/cyclization sequence.
• US6969712B2
  申请人：——

  公开号：US6969712B2

  公开（公告）日：2005-11-29
• Room Temperature Intramolecular Hydro-O-alkylation of Aldehydes:  sp³ C−H Functionalization via a Lewis Acid Catalyzed Tandem 1,5-Hydride Transfer/Cyclization
  作者：Stefan J. Pastine、Dalibor Sames

  DOI：10.1021/ol0522283

  日期：2005.11.1

  The scope and limitations of intramolecular hydro-O-alkylation of aldehyde substrates leading to spiroketals and bicyclic ketals and aminals is reported. The direct transformation of tertiary and sterically hindered secondary sp(3) C-H bonds into C-O bonds under the action of a catalytic amount of a variety of Lewis acids is described. The mechanism of these transformations is proposed to involve a tandem hydride transfer/cyclization sequence.