(R)-tetrahydrofuran-3-yl 4-nitrobenzenesulfonate | 2113708-53-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (R)-tetrahydrofuran-3-yl 4-nitrobenzenesulfonate
• 英文别名: (3R)-Tetrahydro-3-furanyl 4-nitrobenzenesulfonate；[(3R)-oxolan-3-yl] 4-nitrobenzenesulfonate
• CAS: 2113708-53-3
• 化学式: C₁₀H₁₁NO₆S
• 分子量: 273.266
• InChiKey: SZWICZZQOYMFKG-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  107
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  依帕列净杂质 、 (R)-tetrahydrofuran-3-yl 4-nitrobenzenesulfonate 在 potassium carbonate 作用下， 以 正丁醇 为溶剂， 反应 2.0h， 以55 g的产率得到依帕列净
  参考文献：
  名称：

  [EN] A PROCESS FOR THE PREPARATION OF D-GLUCITOL, 1,5-ANHYDRO-1-C-[4-CHLORO-3-[[4- [[(3S)-TETRAHYDRO-3-FURANYL]OXY]PHENYL]METHYL]PHENYL]-, ( 1 S)
  [FR] PROCÉDÉ DE PRÉPARATION DU (1S)-1,5-ANHYDRO-1-C-[4-CHLORO-3-[[4-[[(3S)-TÉTRAHYDRO-3-FURANYL]OXY]PHÉNYL]MÉTHYL]PHÉNYL]-D-GLUCITOL

  摘要：

  本发明涉及一种制备D-葡萄糖醇，1,5-脱水-1-C-[4-氯-3-[[4-[[(3S)-四氢-3-呋喃基)氧)苯基]甲基]苯基]-的过程，化学式为(IS) formula-1。

  公开号：

  WO2018163194A1
• 作为产物：
  描述：

  3-hydroxyfuran 、 对硝基苯磺酰氯 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 以280 g的产率得到(R)-tetrahydrofuran-3-yl 4-nitrobenzenesulfonate
  参考文献：
  名称：

  [EN] A PROCESS FOR THE PREPARATION OF D-GLUCITOL, 1,5-ANHYDRO-1-C-[4-CHLORO-3-[[4- [[(3S)-TETRAHYDRO-3-FURANYL]OXY]PHENYL]METHYL]PHENYL]-, ( 1 S)
  [FR] PROCÉDÉ DE PRÉPARATION DU (1S)-1,5-ANHYDRO-1-C-[4-CHLORO-3-[[4-[[(3S)-TÉTRAHYDRO-3-FURANYL]OXY]PHÉNYL]MÉTHYL]PHÉNYL]-D-GLUCITOL

  摘要：

  本发明涉及一种制备D-葡萄糖醇，1,5-脱水-1-C-[4-氯-3-[[4-[[(3S)-四氢-3-呋喃基)氧)苯基]甲基]苯基]-的过程，化学式为(IS) formula-1。

  公开号：

  WO2018163194A1

文献信息

• [EN] THE PRESENT INVENTION RELATES TO PROCESS FOR THE PREPARATION OF D-GLUCITOL, 1,5- ANHYDRO-1-C-[4-CHLORO-3-[[4-[[(3S)-TETRAHYDRO-3-FURANYL] OXY]PHENYL] METHYL]PHENYL]-, (1S) AND ITS CRYSTALLINE FORMS THEREOF.<br/>[FR] PROCÉDÉ DE PRÉPARATION DE D-GLUCITOL, 1,5- ANHYDRO-1-C-[4-CHLORO-3-[[4-[[(3S)-TÉTRAHYDRO-3-FURANYL] OXY]PHÉNYL] MÉTHYL]PHÉNYL]-, (1S) ET SES FORMES CRISTALLINES
  申请人：MSN LABORATORIES PRIVATE LTD

  公开号：WO2017130217A1

  公开（公告）日：2017-08-03

  The present invention relates to process for the preparation of D-glucitol, 1,5- anhydro-l-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl] methyl]phenyl]-, (1S) formula- 1 and its crystalline forms thereof.

  本发明涉及一种制备D-葡萄糖醇、1,5-脱水-L-C-[4-氯-3-[[4-[(3S)-四氢-3-呋喃基氧基]苯基]甲基]苯基]-（1S）式-1及其晶体形式的方法。
• Processes for the Preparation of SGLT-2 Inhibitors, Intermediates Thereof
  申请人：Emmennar Pharma Private Limited

  公开号：US20180346502A1

  公开（公告）日：2018-12-06

  The present invention relates to novel, improved processes for the preparation of sodium glucose co-transporter 2 (SGLT-2) inhibitors and novel intermediates thereof. More particularly, the present invention relates to a novel, improved process for the preparation of gliflozin compounds such as empagliflozin and dapagliflozin, intermediates thereof. The product obtained from the processes of present invention may be amorphous or crystalline, or in the form of amorphous/crystalline solid dispersions/solutions with pharmaceutically acceptable polymers and preparation process thereof. Also, the products obtained from the present invention may be used for the preparation of medicaments for the prevention and/or treatment of diseases and conditions associated with SGLT-2 inhibition.

  本发明涉及一种新颖的、改进的制备葡萄糖钠共转运蛋白2（SGLT-2）抑制剂及其新颖中间体的方法。更具体地说，本发明涉及一种新颖的、改进的用于制备格列列醇类化合物如恩帕格列醇和达帕格列醇及其中间体的方法。本发明的方法得到的产品可能是非晶态或结晶态，或者以非晶态/结晶态固体分散体/溶液的形式与药用可接受聚合物一起制备。此外，本发明得到的产品可用于制备用于预防和/或治疗与SGLT-2抑制相关的疾病和症状的药物。
• PROCESSES FOR THE PREPARATION OF SGLT-2 INHIBITORS, INTERMEDIATES THEREOF
  申请人：EMMENNAR PHARMA PRIVATE LIMITED

  公开号：US20200331946A1

  公开（公告）日：2020-10-22

  The present invention relates to modified, improved processes for the preparation of sodium glucose co-transporter 2 (SGLT-2) inhibitors and intermediates thereof. More particularly, the present invention relates to improved processes for the preparation of gliflozin compounds such as empagliflozin and dapagliflozin, intermediates thereof. The product obtained from the processes of present invention may be amorphous or crystalline. Also, the products obtained from the present invention may be used for the preparation of medicaments for the prevention and/or treatment of diseases and conditions associated with SGLT-2 inhibition.

  本发明涉及改进的，用于制备钠葡萄糖共转运体2（SGLT-2）抑制剂及其中间体的过程。更具体地，本发明涉及用于制备格列凡诺类化合物，如恩帕格列凡诺和达帕格列凡诺及其中间体的改进过程。本发明所得到的产物可以是非晶态或晶态。此外，本发明所得到的产物可用于制备药物，用于预防和/或治疗与SGLT-2抑制有关的疾病和症状。
• Processes for the preparation of SGLT-2 inhibitors, intermediates thereof
  申请人：Emmennar Pharma Private Limited

  公开号：US10703772B2

  公开（公告）日：2020-07-07

  The present invention relates to novel, improved processes for the preparation of sodium glucose co-transporter 2 (SGLT-2) inhibitors and novel intermediates thereof. More particularly, the present invention relates to a novel, improved process for the preparation of gliflozin compounds such as empagliflozin and dapagliflozin, intermediates thereof. The product obtained from the processes of present invention may be amorphous or crystalline, or in the form of amorphous/crystalline solid dispersions/solutions with pharmaceutically acceptable polymers and preparation process thereof. Also, the products obtained from the present invention may be used for the preparation of medicaments for the prevention and/or treatment of diseases and conditions associated with SGLT-2 inhibition.

  本发明涉及制备钠葡萄糖共转运体2（SGLT-2）抑制剂及其新型中间体的新型改进工艺。更具体地说，本发明涉及一种制备格列洛嗪化合物（如empagliflozin和dapagliflozin）及其中间体的新型改进工艺。从本发明工艺中获得的产品可以是无定形或结晶，或以无定形/结晶固体分散体/溶液的形式与药学上可接受的聚合物及其制备工艺一起存在。此外，本发明所得产品还可用于制备预防和/或治疗与 SGLT-2 抑制有关的疾病和病症的药物。
• Process for the preparation of D-glucitol, 1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl] oxy]phenyl] methyl] phenyl]-, (1S) and its crystalline forms thereof
  申请人：MSN LABORATORIES PRIVATE LIMITED

  公开号：US10913762B2

  公开（公告）日：2021-02-09

  The present invention relates to process for the preparation of D-glucitol, 1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl] methyl]phenyl]-, (1S) formula-1 and its crystalline forms thereof.

  本发明涉及 D-葡萄糖醇、1,5-脱水-1-C-[4-氯-3-[[4-[[(3S)-四氢-3-呋喃基]氧基]苯基]甲基]苯基]-、（1S）式-1 及其结晶形式的制备工艺。