[4]piperidylmethyl-malonic acid | 304873-70-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: [4]piperidylmethyl-malonic acid
• 英文别名: [4]Piperidylmethyl-malonsaeure；2-(4-Piperidinylmethyl)propanedioic acid；2-(piperidin-4-ylmethyl)propanedioic acid
• CAS: 304873-70-9
• 化学式: C₉H₁₅NO₄
• 分子量: 201.222
• InChiKey: REZBAEQJAYELJR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.1
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  86.6
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 盐酸 、 铂 作用下， 生成 [4]piperidylmethyl-malonic acid
  参考文献：
  名称：

  Rubzow et al., Zhurnal Obshchei Khimii, 1953, vol. 23, p. 963,967; engl. Ausg. S. 1001, 1004

  摘要：

  DOI：

文献信息

• [EN] PIPERIDINE DERIVATIVES USEFUL AS GPR119 AGONISTS<br/>[FR] DÉRIVÉS DE LA PIPÉRIDINE UTILISÉS COMME AGONISTES DU RÉCEPTEUR GPR119
  申请人：MERCK SHARP & DOHME

  公开号：WO2013062837A1

  公开（公告）日：2013-05-02

  Substituted piperidine compounds and pharmaceutically acceptable salts thereof are disclosed. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to G-protein coupled receptor agonists. In particular, the present invention is directed to agonists of GPR 119 that are useful for the treatment of diabetes, especially type 2 diabetes, obesity, the metabolic syndrome and related diseases and conditions.

  本发明涉及替代哌啶化合物及其药用盐。药物组合物和治疗方法也包括在内。本发明涉及G蛋白偶联受体激动剂。具体而言，本发明涉及对GPR 119的激动剂，适用于治疗糖尿病，特别是2型糖尿病、肥胖、代谢综合征以及相关疾病和病况。
• PROCESS AND INTERMEDIATES FOR PRODUCTION OF DONEPEZIL AND RELATED COMPOUNDS
  申请人：Finetech Ltd

  公开号：EP1129073A2

  公开（公告）日：2001-09-05
• US6492522B1
  申请人：——

  公开号：US6492522B1

  公开（公告）日：2002-12-10
• [EN] NOVEL PROCESS AND INTERMEDIATES FOR PRODUCTION OF DONEPEZIL AND RELATED COMPOUNDS<br/>[FR] NOUVEAU PROCEDE ET INTERMEDIAIRES POUR LA PRODUCTION DE DONEPEZIL ET DE SES COMPOSES APPARENTES
  申请人：FINETECH LTD

  公开号：WO2000009483A2

  公开（公告）日：2000-02-24

  The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R1 is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; 4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-(φ-aralkyl)-4-piperidyl; 4-pyridyl; R?4, R5, R6 and R7¿ are identical or different and each represents hydrogen, straight-chain or branched alkyl, aryl, hydroxy, alkoxy, aryloxy, benzyloxy, acyloxy, alkylthio, arylthio, benzylthio, acylamino, phthalimido or halogen; n is 1, 2 or 3; m is 1, 2, 3, 4 or 5. This process comprises cyclisation of a compound of formula (II) or salts thereof, wherein R?1, R4, R5, R6 and R7¿, m and n are as defined above; R2 is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R3 is selected from a derivatised or non-derivatised carboxyl, cyano or N-substituted aminocarbonyl groups, optionally in the presence of acids and/or solvents. One of the most potent acetylcholinesterase inhibitors of the class of compounds prepared according to the present invention is donepezil.