6-Hydroxy-2-(4-hydroxyphenyl)-3-(4-(2-piperidinoethoxy)-benzoyl]benzo[b]thiophene Hydrochloride 1,2-Dichloroethane

• 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)-3-(4-(2-piperidinoethoxy)-benzoyl]benzo[b]thiophene Hydrochloride 1,2-Dichloroethane
• 英文别名: 1,2-dichloroethane;[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-piperidin-1-ylethoxy)phenyl]methanone;hydrochloride
• 化学式: C30H32Cl3NO4S
• 分子量: 609.0
• InChiKey: APMJBTGDXWLDED-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.96
• 重原子数：
  39
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  98.2
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  盐酸雷洛昔芬 、 1,2-二氯乙烷 生成 6-Hydroxy-2-(4-hydroxyphenyl)-3-(4-(2-piperidinoethoxy)-benzoyl]benzo[b]thiophene Hydrochloride 1,2-Dichloroethane
  参考文献：
  名称：

  Benzothiophenes, formulations containing same, and methods

  摘要：

  该发明提供了I式化合物及其药学上可接受的盐和溶剂化物，其特征在于该化合物呈颗粒状，并具有特定的尺寸范围。本发明还提供了含有或使用I式化合物制备的药物组合物，并使用这些化合物缓解人类病理学，包括骨质疏松症、血清脂质降低和乳腺癌。

  公开号：

  US06894064B2

文献信息

• [EN] PROCESS FOR THE SYNTHESIS OF BENZO[b]THIOPHENES<br/>[FR] PROCEDE DE SYNTHESE DE BENZO[b]THIOPHENES
  申请人：ELI LILLY AND COMPANY

  公开号：WO1996040677A1

  公开（公告）日：1996-12-19

  (EN) The present invention is directed to new processes for the synthesis of 2-aryl benzo[b]thiophenes.(FR) L'invention concerne de nouveaux procédés de synthèse de 2-arylbenzo[b]thiophènes.

  这项发明涉及合成2-芳基苯并[b]噻吩的新工艺。
• Non-solvated crystalline 6-hydroxy-2- (4-hydroxyphenyl) -3- [4- (2-piperidinoethoxy) benzoyl] benzo [b] thiophene hydrochloride
  申请人：——

  公开号：US20020173645A1

  公开（公告）日：2002-11-21

  The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.

  本发明涉及用于制备2-芳基-6-羟基-3-[4-(2-氨基乙氧基)苯甲酰基]苯并[b]噻吩的化学过程。本发明还涉及6-羟基-2-(4-羟基苯基)-3-[4-(2-哌啶基乙氧基)苯甲酰基]苯并[b]噻吩盐的晶体溶剂和非溶剂晶体形式，以及它们的制备方法。
• Synthesis of 3-\x9b4-(2-aminoethoxy)benzoyl!-2-aryl-6-hydroxybenzo
  申请人：Eli Lilly and Company

  公开号：US05731327A1

  公开（公告）日：1998-03-24

  The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-\x9b4-(2-aminoethoxy)benzoyl!benzo\x9bb!-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-\x9b4-(2-piperidinoethoxy)benzoyl!-benzo\x9bb!th iophene hydrochloride, as well as processes for their preparation.

  本发明涉及用于制备2-芳基-6-羟基-3-（4-（2-氨基乙氧基）苯甲酰基）苯并[b]噻吩的化学过程。本发明还涉及6-羟基-2-（4-羟基苯基）-3-（4-哌啶基乙氧基）苯甲酰基-苯并[b]噻吩盐酸盐的晶体溶剂和非溶剂晶体形式，以及它们的制备方法。
• Synthesis of 3-&lsqb;4-(2-aminoethoxy)-benzoyl&rsqb;-2-aryl-6-hydroxybenzo&lsqb;b&rsqb;thiophenes
  申请人：Eli Lilly and Company

  公开号：US06399778B1

  公开（公告）日：2002-06-04

  The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.

  本发明涉及用于制备2-芳基-6-羟基-3-[4-(2-氨基乙氧基)苯甲酰基]苯并[b]噻吩的化学过程。本发明还涉及6-羟基-2-(4-羟基苯基)-3-[4-(2-哌啶基乙氧基)苯甲酰基]-苯并[b]噻吩盐的晶体溶剂和非溶剂晶体形式，以及它们的制备方法。
• Benzothiophenes formulations containing same and methods
  申请人：Eli Lilly and Company

  公开号：US06458811B1

  公开（公告）日：2002-10-01

  This invention provides compounds of formula I and pharmaceutically acceptable salts and solvates thereof, characterized that the compound is in particulate form and having a specific size range. The present invention further provides pharmaceutical compositions containing or formulated using compounds of formula I, and the use of such compounds for alleviating human pathologies, including osteoporosis, serum lipid lowering, and breast cancer.

  本发明提供了公式I的化合物及其药学上可接受的盐和溶剂化物，其特征在于该化合物呈颗粒状，并具有特定的尺寸范围。本发明还提供了含有或使用公式I化合物制备的制剂的药物组合物，并且使用这种化合物缓解人类病理状况，包括骨质疏松症、血清脂质降低和乳腺癌。