2-[4-Chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-[4-Chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
• 化学式: C₂₁H₂₅ClO₆
• 分子量: 408.9
• InChiKey: JVHXJTBJCFBINQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  99.4
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• Novel aromatic fluoroglycoside derivatives, pharmaceuticals comprising said compounds and the use thereof
  申请人：FRICK Wendelin

  公开号：US20110059910A1

  公开（公告）日：2011-03-10

  The invention relates to substituted aromatic fluoroglycoside derivatives, and to the physiologically compatible salts and physiologically functional derivatives thereof. The invention also relates to methods of lowering blood sugar and the treatment of type I and type II diabetes.

  这项发明涉及取代芳香族氟糖苷衍生物，以及其生理兼容盐和生理功能衍生物。该发明还涉及降低血糖和治疗I型和II型糖尿病的方法。
• [EN] PREMIX OF DAPAGLIFLOZIN AND PROCESS FOR THE PREPARATION THEREOF<br/>[FR] PRÉMÉLANGE DE DAPAGLIFLOZINE ET SON PROCÉDÉ DE PRÉPARATION
  申请人：LUPIN LTD

  公开号：WO2017118945A1

  公开（公告）日：2017-07-13

  The present invention relates to a premix of dapagliflozin with lactose, processes for its preparation, and pharmaceutical composition thereof. The invention also relates to a process for the preparation of an amorphous dapagliflozin and crystalline dapagliflozin propanediol hydrate.

  本发明涉及带有乳糖的达格列凡司琼的预混物，其制备方法以及其制药组合物。该发明还涉及一种制备非晶态达格列凡司琼和结晶达格列凡司琼丙二醇水合物的方法。
• [EN] PROCESS FOR THE PREPARATION OF DAPAGLIFLOZIN<br/>[FR] PROCÉDÉ DE PRÉPARATION DE DAPAGLIFLOZINE
  申请人：INDOCO REMEDIES LTD

  公开号：WO2018142422A1

  公开（公告）日：2018-08-09

  The present invention discloses a novel process for the preparation of Dapagliflozin (S)-propylene glycol hydrate of Formula II. (Formula II)

  本发明公开了一种制备达格列净(S)-丙二醇水合物的新工艺，其化学式为II。
• [EN] A NOVEL PROCESS FOR PREPARING (2S,3R,4R,5S,6R)-2-[4-CHLORO-3-(4-ETHOXYBENZYL)PHENY 1] -6-(HY DROXY METHYL)TETRAHYDRO-2H-PY RAN-3,4,5-TRIOL AND ITS AMORPHOUS FORM<br/>[FR] NOUVEAU PROCÉDÉ DE PRÉPARATION DE (2S,3R,4R,5S,6R)-2-[4-CHLORO-3-(4-ÉTHOXYBENZYL)PHÉNYL]-6-(HYDROXYMÉTHYL)TÉTRAHYDRO-2H-PYRAN-3,4,5-TRIOL ET SA FORME AMORPHE
  申请人：HARMAN FINOCHEM LTD

  公开号：WO2016147197A1

  公开（公告）日：2016-09-22

  The present invention discloses the process for preparation of (2S,3R,4R,5S,6R)-2-[4- chloro-3-(4-ethoxybenzyl)phenyl]-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol and its amorphous form.

  本发明揭示了制备(2S,3R,4R,5S,6R)-2-[4-氯-3-(4-乙氧基苯基)苄基]苯基]-6-(羟甲基)四氢-2H-吡喃-3,4,5-三醇及其非晶态形式的过程。
• [EN] NOVEL PIPECOLIC ACID CO-CRYSTALS OF DAPAGLIFLOZIN AND PROCESS FOR THE PREPARATION THEREOF<br/>[FR] NOUVEAU CO-CRISTAUX D'ACIDE PIPÉCOLIQUE DE DAPAGLIFLOZINE ET LEUR PROCÉDÉ DE PRÉPARATION
  申请人：HARMAN FINOCHEM LTD

  公开号：WO2017060925A1

  公开（公告）日：2017-04-13

  The present invention discloses the process for preparation of (2S,3R,4R,5S,6R)- 2-[4-chloro-3-(4-ethoxybenzyl)phenyl]-6-(hydroxymethyl)tetrahydro-2H-pyran- 3,4,5-trioland its amorphous form. The invention further discloses novelco- crystals of dapagliflozin,and process for preparation thereof. The invention further discloses novel intermediateAcetic acid 4,5-diacetoxy-6-acetoxymethyl-2-R1-2- [4-chloro-3-(4-ethoxy-benzyl)-phenyl]-tetrahydro-pyran-3-yl ester, wherein R1 is allyl or 2-prop-2ynyl useful for preparation 2-R1-2-[4-Chloro-3-(4-ethoxy- benzyl)-phenyl]-6-hydroxymethyl-tetrahydro-pyran-3,4,5-triol.

  本发明揭示了制备(2S,3R,4R,5S,6R)-2-[4-氯-3-(4-乙氧基苯基)苄基]苯基]-6-(羟甲基)四氢-2H-吡喃-3,4,5-三醇及其非晶态形式的过程。本发明还揭示了达格列净的新型共晶体及其制备方法。本发明还揭示了新型中间体乙酸4,5-二乙酰氧基-6-乙酰氧甲基-2-R1-2-[4-氯-3-(4-乙氧基苯基)苄基]-四氢-吡喃-3-基酯，其中R1为烯丙基或2-丙-2-炔基，用于制备2-R1-2-[4-氯-3-(4-乙氧基苯基)苄基]-6-羟甲基-四氢-吡喃-3,4,5-三醇。