Alendronic acid monohydrate | 138624-11-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机膦酸及其衍生物
• 英文名称: Alendronic acid monohydrate
• 英文别名: (4-amino-1-hydroxy-1-phosphonobutyl)phosphonic acid;hydrate
• CAS: 138624-11-0
• 化学式: C₄H₁₃NO₇P₂*H₂O
• 分子量: 267.113
• InChiKey: AQAZLLYAEFBJMU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.1
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  162
• 氢给体数：
  7
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  Alendronic acid monohydrate 、 sodium hydroxide 在 乙醇 作用下， 以 乙醇 为溶剂， 25.0~50.0 ℃ 、266.62 kPa 条件下， 反应 34.0h， 以to give 26.2 g of alendronate sodium的产率得到sodium alendronate
  参考文献：
  名称：

  Hydrate forms of alendronate sodium, processes for manufacture thereof, and pharmaceutical compositions thereof

  摘要：

  本发明公开了一种阿伦膦酸钠的新水合物形式，其水含量在约1％至约12％之间，并公开了其制造方法。还公开了阿伦膦酸钠B，D，E，F，G和H的新晶体形式以及制造它们的方法。这些阿伦膦酸钠的新形式适用于纳入制药组合物中，用于治疗骨疾病中的骨吸收。

  公开号：

  US06696601B2
• 作为产物：
  描述：

  4-氨基丁酸 、 亚磷酸 、 五氯化磷 、 甲烷磺酸 生成 Alendronic acid monohydrate
  参考文献：
  名称：

  KIECZYKOWSKI, GERARD R.;MELILLO, DAVID G.;JOBSOU, RONALD B.

  摘要：

  DOI：

文献信息

• Novel process for making bisphosphonic acids using diluents other than halogenated hydrocarbons
  申请人：Lidor-Hadas Rami

  公开号：US20060128960A1

  公开（公告）日：2006-06-15

  Provided is a novel method of making bisphosphonic acids, e.g. risedronic acid, including the step of combining a carboxylic acid, phoshorous acid, and a halophosphorous compound in the presence of a diluent that is an aromatic hydrocarbon or a silicone fluid. When the diluent is an aromatic hydrocarbon, a inert support or ortho-phosphoric acid codiluent is advantageously included.

  提供了一种制备双膦酸的新方法，例如利塞酮酸，包括在芳香烃或硅流体的稀释剂存在下，将羧酸、磷酸和卤磷化合物结合的步骤。当稀释剂是芳香烃时，可以优选地包括惰性支撑物或邻-磷酸共溶剂。
• Novel hydrate forms of alendronate sodium, processes for manufacture thereof, and pharmaceutical compositions thereof
  申请人：——

  公开号：US20030065214A1

  公开（公告）日：2003-04-03

  New hydrate forms of alendronate sodium, having water content of between about one and about twelve percent, and processes for their manufacture, are disclosed. New crystalline forms of alendronate sodium B, D, E, F, G and H, and processes for manufacturing them, are also disclosed. These new forms of alendronate sodium are suitable for incorporation into pharmaceutical compositions for combating bone resorption in bone diseases.

  本发明公开了一种阿伦膦酸钠的新水合物形式，其水含量在约1％至约12％之间，并公开了其制造方法。本发明还公开了阿伦膦酸钠B、D、E、F、G和H的新晶体形式及其制造方法。这些阿伦膦酸钠的新形式适用于纳入制药组合物中，以用于治疗骨疾病中的骨吸收。
• Process for the preparation of solid oral dosage forms comprising alendronic acid
  申请人：Unipharm Ltd.

  公开号：US06465017B1

  公开（公告）日：2002-10-15

  The present invention relates to a process for preparing solid oral dosage forms e.g. tablets,capsules,coated tablets/capsules, etc. comprising as active ingredient 4-amino-1-hydroxybutylidene-1, 1-biphosphonic acid or one of its pharmaceutically acceptable salts (“Alendronic acid”). It comprises the free acid or one of its pharmaceutically acceptable salts. The process is characterized by granulating pharmaceutical carriers with an aqueous solution of Alendronic acid which is solubilized with the aid of alkaline hydroxides or alkaline salts. The oral dosage forms obtained by this process are less irritating to the digestive system than oral dosage forms obtained by conventional processes. The present invention also relates to tablets and to capsules prepared by said process.

  本发明涉及一种制备固体口服剂型（例如片剂、胶囊、包衣片剂/胶囊等）的工艺，其中包括4-氨基-1-羟基丁烯基-1,1-双膦酸或其药用可接受盐（“阿仑膦酸”）作为活性成分。它包括游离酸或其药用可接受盐。该工艺的特点是将药用载体与碱性氢氧化物或碱性盐辅助溶解的阿仑膦酸水溶液颗粒化。通过该工艺获得的口服剂型对消化系统的刺激性比传统工艺获得的口服剂型小。本发明还涉及通过该工艺制备的片剂和胶囊。
• Process for making bisphosphonic acids using diluents other than halogenated hydrocarbons
  申请人：Teva Pharmaceutical Industries, Ltd.

  公开号：US07038083B2

  公开（公告）日：2006-05-02

  Provided is a novel method of making bisphosphonic acids, e.g. risedronic acid, including the step of combining a carboxylic acid, phoshorous acid, and a halophosphorous compound in the presence of a diluent that is an aromatic hydrocarbon or a silicone fluid. When the diluent is an aromatic hydrocarbon, a inert support or ortho-phosphoric acid codiluent is advantageously included.

  提供了一种制备双膦酸的新方法，例如利塞酸，其中包括在芳香族碳氢化合物或硅流体的存在下将羧酸、磷酸和卤代磷化合物相结合的步骤。当芳香族碳氢化合物是稀释剂时，优选地包括惰性支撑物或邻磷酸酯共溶剂。
• Novel Process For Making Bisphosphonic Acids Using Diluents Other Than Halogenated Hydrocarbons
  申请人：Lidor-Hadas Rami

  公开号：US20090209763A1

  公开（公告）日：2009-08-20

  Provided is a novel method of making bisphosphonic acids, e.g. risedronic acid, including the step of combining a carboxylic acid, phosphorous acid, and a halophosphorous compound in the presence of a diluent that is an aromatic hydrocarbon or a silicone fluid. When the diluent is an aromatic hydrocarbon, an inert support or ortho-phosphoric acid codiluent is advantageously included.

  提供了一种制备双磷酸盐酸的新方法，例如利塞酸，包括在芳香烃或硅流体存在的稀释剂的情况下，结合羧酸、磷酸和卤代磷化合物的步骤。当稀释剂为芳香烃时，优选地包括惰性支撑物或邻二磷酸共溶剂。