(2S)-2-(cyclopropylmethoxymethyl)pyrrolidine | 1187303-86-1

• 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: (2S)-2-(cyclopropylmethoxymethyl)pyrrolidine
• CAS: 1187303-86-1
• 化学式: C₉H₁₇NO
• 分子量: 155.24
• InChiKey: GLVITWRCASQHHS-VIFPVBQESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  11
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2S)-2-(cyclopropylmethoxymethyl)pyrrolidine 、 Boc-(R)-3-氨基-4-(2,4,5-三氟苯基)丁酸 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  From lead to preclinical candidate: Optimization of β-homophenylalanine based inhibitors of dipeptidyl peptidase IV

  摘要：

  A series of highly potent and selective inhibitors of DPP-4 was optimized for ADMET properties. The effort resulted in the discovery of inhibitor 1g, that exhibits excellent efficacy in an oral glucose tolerance test and an attractive pharmacokinetic profile. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.06.036
• 作为产物：
  描述：

  tert-butyl (2S)-2-(cyclopropylmethoxymethyl)pyrrolidine-1-carboxylate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 (2S)-2-(cyclopropylmethoxymethyl)pyrrolidine
  参考文献：
  名称：

  From lead to preclinical candidate: Optimization of β-homophenylalanine based inhibitors of dipeptidyl peptidase IV

  摘要：

  A series of highly potent and selective inhibitors of DPP-4 was optimized for ADMET properties. The effort resulted in the discovery of inhibitor 1g, that exhibits excellent efficacy in an oral glucose tolerance test and an attractive pharmacokinetic profile. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.06.036

文献信息

• Dpp-Iv Inhibitors
  申请人：Edwards Paul John

  公开号：US20080027035A1

  公开（公告）日：2008-01-31

  The invention relates to compounds of formula (I) wherein Z, R 1-5 , X, n, A 1 and A 2 have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.

  本发明涉及式（I）的化合物，其中Z，R1-5，X，n，A1和A2的含义如所述及权利要求中所述。所述化合物可用作DPP-IV抑制剂。本发明还涉及制备这种化合物以及其作为药物的生产和使用。
• DPP-IV INHIBITORS
  申请人：Santhera Pharmaceuticals (Schweiz) AG

  公开号：EP1613304B1

  公开（公告）日：2007-09-12
• [EN] DPP-IV INHIBITORS<br/>[FR] INHIBITEURS DPP-IV
  申请人：GRAFFINITY PHARMACEUTICALS AG

  公开号：WO2005056003A1

  公开（公告）日：2005-06-23

  The invention relates to compounds of formula (I): (I), wherein Z, R1-5, X, n, A1 and A2 have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and thereof as medicament.
• From lead to preclinical candidate: Optimization of β-homophenylalanine based inhibitors of dipeptidyl peptidase IV
  作者：Sonja Nordhoff、Meritxell López-Canet、Barbara Hoffmann-Enger、Stephan Bulat、Silvia Cerezo-Gálvez、Oliver Hill、Claudia Rosenbaum、Christian Rummey、Meinolf Thiemann、Victor G. Matassa、Paul J. Edwards、Achim Feurer

  DOI：10.1016/j.bmcl.2009.06.036

  日期：2009.8

  A series of highly potent and selective inhibitors of DPP-4 was optimized for ADMET properties. The effort resulted in the discovery of inhibitor 1g, that exhibits excellent efficacy in an oral glucose tolerance test and an attractive pharmacokinetic profile. (C) 2009 Elsevier Ltd. All rights reserved.