[6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-4-[2-(1-piperidinyl)ethoxy]phenyl DL-lactate | 676635-78-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-4-[2-(1-piperidinyl)ethoxy]phenyl DL-lactate
• 英文别名: [6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-piperidin-1-ylethoxy)phenyl]methanone;2-hydroxypropanoic acid
• CAS: 676635-78-2
• 化学式: C₃H₆O₃*C₂₈H₂₇NO₄S
• 分子量: 563.672
• InChiKey: TYOSMNSOONUCQD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.53
• 重原子数：
  40
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  156
• 氢给体数：
  4
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  乳酸 、 盐酸雷洛昔芬 在 氢氧化钾 作用下， 以 异丙醇 为溶剂， 反应 20.25h， 以83.9%的产率得到[6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-4-[2-(1-piperidinyl)ethoxy]phenyl DL-lactate
  参考文献：
  名称：

  [EN] NOVEL RALOXIFENE ACID ADDITION SALTS AND/OR SOLVATES THEREOF, IMPROVED METHOD FOR PURIFICATION OF SAID RALOXIFENE ACID ADDITION SALTS AND/OR SOLVATES THEREOF AND PHARMACEUTICAL COMPOSITIONS COMPRISING THESE
  [FR] NOUVEAUX SELS D'ADDITION ACIDES DE RALOXIFENE ET/OU SOLVATES DE CEUX-CI, PROCEDE AMELIORE PERMETTANT LA PURIFICATION DE CES SELS D'ADDITION ACIDES ET/OU DE CES SOLVATES, ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT

  摘要：

  公开号：

  WO2004029046A3

文献信息

• METHOD FOR SALT PREPARATION
  申请人：Wieser Josef

  公开号：US20100204470A1

  公开（公告）日：2010-08-12

  The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide.

  本发明提供了一种新的制备和结晶药物化合物或其中间体的盐酸盐、溴化盐或碘化盐的方法，在该方法中，将碱或其酸加成盐在溶剂中与三烷基硅基卤化物反应。
• Novel raloxifene acid additon salts and/or solvates thereof, improved method for purification of said raloxifene acid addition salts and/or solvates thereof and pharmaceutical compositions comprising these
  申请人：Karup Leo Gunnar

  公开号：US20060154966A1

  公开（公告）日：2006-07-13

  Raloxifene acid addition salts or solvates thereof, having improved dissolution properties in media comprising hydrochloric acid are described, compared with similar preparations based on raloxifene or raloxifene hydrochloride. The disclosed acid addition salts or solvates thereof show an improved bioavailability in media comprising hydrochloric acid, such as the gastric juice. The acid addition salts or solvates thereof are addition salts or solvates of raloxifene and a pharmaceutical acceptable acid selected among succinic acid, lactic acid, malonic acid or sulphuric acid. Further, crystalline forms of the raloxifene salts and solvates thereof are disclosed. The raloxifene acid addition salts and/or solvates thereof are useful for the preparation of pharmaceutical composition for oral administration capable of fast and reliable release of the active ingredients in the stomach of the patient, in particular for the treatment of cancer or osteoporosis, or for inhibiting cartilage degradation. A new method for preparation of raloxifene lactate is also disclosed.

  与基于雷洛昔芬或盐酸雷洛昔芬的类似制剂相比，雷洛昔芬酸加成盐或其溶解物在含有盐酸的介质中具有更好的溶解特性。所公开的酸加成盐或其溶解物在含有盐酸的介质（如胃液）中显示出更好的生物利用度。其酸加成盐或溶解物是雷洛昔芬和选自琥珀酸、乳酸、丙二酸或硫酸的药物可接受酸的加成盐或溶解物。此外，还公开了雷洛昔芬盐及其溶液的结晶形式。雷洛昔芬酸加成盐和/或其溶解物可用于制备口服药物组合物，能够在患者胃中快速、可靠地释放活性成分，特别是用于治疗癌症或骨质疏松症，或用于抑制软骨降解。此外，还公开了一种制备乳酸雷洛昔芬的新方法。
• NOVEL RALOXIFENE ACID ADDITION SALTS AND/OR SOLVATES THEREOF, IMPROVED METHOD FOR PURIFICATION OF SAID RALOXIFENE ACID ADDITION SALTS AND/OR SOLVATES THEREOF AND PHARMACEUTICAL COMPOSITIONS COMPRISING THESE
  申请人：A/S GEA Farmaceutisk Fabrik

  公开号：EP1546138A2

  公开（公告）日：2005-06-29
• RALOXIFENE L-LACTATE OR A HEMIHYDRATE THEREOF, THEIR USES, PHARMACEUTICAL COMPOSITIONS AND PREPARATION PROCESSES
  申请人：A/S GEA Farmaceutisk Fabrik

  公开号：EP1546138B1

  公开（公告）日：2012-01-18
• NEW METHOD FOR SALT PREPARATION
  申请人：Sandoz AG

  公开号：EP2032521A2

  公开（公告）日：2009-03-11