[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]-morpholin-4-ylmethanone | 727722-98-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: [(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]-morpholin-4-ylmethanone
• CAS: 727722-98-7
• 化学式: C₁₀H₁₇NO₄
• 分子量: 215.249
• InChiKey: KCLJRENHDBIOGX-MRVPVSSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  48
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  [(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]-morpholin-4-ylmethanone 在 magnesium 作用下， 以 四氢呋喃 为溶剂， 反应 0.33h， 生成
  参考文献：
  名称：

  Stereocontrolled synthesis of (1S)-1-(1H-imidazol-4-yl)-1-(6-methoxy-2-naphthyl)-2-methylpropan-1-ol as a potent C17,20-lyase inhibitor

  摘要：

  An efficient stereocontrolled synthesis of the Potent C-17.20-lyase inhibitor, (1S)-1-(1H-imidazol-4-yl)-1-(6-methoxy-2-naphthyl)-2-methyl-1-propanol 1, has been established. The stereogenic center of 1 was successfully constructed by a highly diastereoselective Grignard reaction of 2, while a subsequent imidazole ring annulation afforded 1 in an enantiomerically pure form. The procedure enables a practical synthesis of 1 that can be conveniently carried out on a multigram scale. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetasy.2004.02.035
• 作为产物：
  描述：

  吗啉 、 (R)-(+)-2,2-二甲基-1,3-二氧戊环-4-羧酸甲酯 反应 16.0h， 以71%的产率得到[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]-morpholin-4-ylmethanone
  参考文献：
  名称：

  Stereocontrolled synthesis of (1S)-1-(1H-imidazol-4-yl)-1-(6-methoxy-2-naphthyl)-2-methylpropan-1-ol as a potent C17,20-lyase inhibitor

  摘要：

  An efficient stereocontrolled synthesis of the Potent C-17.20-lyase inhibitor, (1S)-1-(1H-imidazol-4-yl)-1-(6-methoxy-2-naphthyl)-2-methyl-1-propanol 1, has been established. The stereogenic center of 1 was successfully constructed by a highly diastereoselective Grignard reaction of 2, while a subsequent imidazole ring annulation afforded 1 in an enantiomerically pure form. The procedure enables a practical synthesis of 1 that can be conveniently carried out on a multigram scale. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetasy.2004.02.035

文献信息

• [EN] COMPOUNDS HAVING TRPV1 ANTAGONISTIC ACTIVITY AND USES THEREOF<br/>[FR] COMPOSÉS PRÉSENTANT UNE ACTIVITÉ ANTAGONISTE DES TRPV1 ET LEURS UTILISATIONS
  申请人：SHIONOGI & CO

  公开号：WO2011162409A1

  公开（公告）日：2011-12-29

  The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.

  该发明涉及化合物I的公式和其药用可接受的衍生物，包含有效量的化合物I或其药用可接受的衍生物的组合物，以及治疗或预防疼痛、尿失禁、溃疡、炎症性肠病和肠易激综合征等疾病的方法，包括向需要的动物施用化合物I或其药用可接受的衍生物的有效量。
• COMPOUNDS HAVING TRPV1 ANTAGONISTIC ACTIVITY AND USES THEREOF
  申请人：Kurose Noriyuki

  公开号：US20130123239A1

  公开（公告）日：2013-05-16

  The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.

  本发明涉及公式I的化合物及其药学上可接受的衍生物，包括含有公式I的化合物或其药学上可接受的衍生物的有效量的组合物，并且涉及治疗或预防疼痛、尿失禁、溃疡、炎症性肠病和肠易激综合征等疾病的方法，其中向需要治疗的动物中给予公式I的化合物或其药学上可接受的衍生物的有效量。
• US8921373B2
  申请人：——

  公开号：US8921373B2

  公开（公告）日：2014-12-30