(2S,3R,4R,5S)-2-(4-chloro-3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)phenyl)-6-methoxytetrahydro-2H-pyran-3,4,5-triol | 1415468-95-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (2S,3R,4R,5S)-2-(4-chloro-3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)phenyl)-6-methoxytetrahydro-2H-pyran-3,4,5-triol
• 英文别名: (2S,3R,4R,5S)-2-(4-Chloro-3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)phenyl)-6-methoxytetrahydro-2H-pyran-3,4,5-triol；(2S,3R,4R,5S)-2-[4-chloro-3-(2,3-dihydro-1,4-benzodioxin-6-ylmethyl)phenyl]-6-methoxyoxane-3,4,5-triol
• CAS: 1415468-95-9
• 化学式: C₂₁H₂₃ClO₇
• 分子量: 422.862
• InChiKey: CRWDMTYWPUBEDF-AUGMSIGLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  97.6
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  (2S,3R,4R,5S)-2-(4-chloro-3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)phenyl)-6-methoxytetrahydro-2H-pyran-3,4,5-triol 、 乙酸酐 在 吡啶 、 4-二甲氨基吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 12.0h， 以87%的产率得到(2S,3S,4R,5S)-2-(4-chloro-3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)phenyl)-6-methoxytetrahydro-2H-pyran-3,4,5-triyl triacetate
  参考文献：
  名称：

  JP5876570

  摘要：

  公开号：
• 作为产物：
  描述：

  (4-chloro-3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)phenyiy(3aS,5R,6S,6aS)-6-hydroxy-2,2-dimethyltetrahydroruro[3,2-d][1,3]dioxol-5-yr)methanone 在 盐酸 、 sodium tetrahydroborate 、 cerium(III) chloride heptahydrate 、 乙酰氯 作用下， 以 甲醇 、 水 为溶剂， 反应 3.0h， 生成 (2S,3R,4R,5S)-2-(4-chloro-3-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)phenyl)-6-methoxytetrahydro-2H-pyran-3,4,5-triol
  参考文献：
  名称：

  JP5876570

  摘要：

  公开号：

文献信息

• NOVEL DIPHENYLMETHANE DERIVATIVES AS SGLT2 INHIBITORS
  申请人：Choi Soongyu

  公开号：US20140088079A1

  公开（公告）日：2014-03-27

  The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.

  本发明涉及一种具有二苯甲烷基团的化合物，其具有对存在于肠和肾中的钠依赖性葡萄糖共转运体2（SGLT2）的抑制活性，以及包含该化合物作为活性成分的制药组合物，用于预防或治疗代谢性疾病，尤其是糖尿病。本发明还提供了一种制备该化合物的方法，以及使用该化合物预防或治疗代谢性疾病，尤其是糖尿病的方法。
• Diphenylmethane derivatives as SGLT2 inhibitors
  申请人：GREEN CROSS CORPORATION

  公开号：US09371303B2

  公开（公告）日：2016-06-21

  A compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney is disclosed. A pharmaceutical composition including the compound as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes is disclosed. A method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound is provided.

  本发明揭示了一种含有二苯甲烷基团的化合物，该化合物具有抑制存在于肠和肾中的钠依赖性葡萄糖共转运体2（SGLT2）的活性。本发明还揭示了一种包括该化合物作为活性成分的制药组合物，该组合物可用于预防或治疗代谢紊乱，特别是糖尿病。本发明还提供了一种制备该化合物的方法，以及使用该化合物预防或治疗代谢紊乱，特别是糖尿病的方法。
• US9034921B2
  申请人：——

  公开号：US9034921B2

  公开（公告）日：2015-05-19
• US9371303B2
  申请人：——

  公开号：US9371303B2

  公开（公告）日：2016-06-21
• [EN] NOVEL DIPHENYLMETHANE DERIVATIVES AS SGLT2 INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS DE DIPHÉNYLMÉTHANE EN TANT QU'INHIBITEURS DE SGLT2
  申请人：GREEN CROSS CORP

  公开号：WO2012165914A2

  公开（公告）日：2012-12-06

  The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.