R-普拉克索盐酸盐 | 104632-27-1

• 物质功能分类: 分析化学 - 标准品 - 药典标准品和杂质标准品
• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: R-普拉克索盐酸盐
• 中文别名: 普拉克索杂质D
• 英文名称: (R)-Pramipexole Dihydrochloride
• 英文别名: (6R)-6-N-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine;dihydrochloride
• CAS: 104632-27-1
• 化学式: C10H19Cl2N3S
• 分子量: 284.2
• InChiKey: QMNWXHSYPXQFSK-XCUBXKJBSA-N

物化性质

• 溶解度：
  H2O：>15mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  2.43
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  79.2
• 氢给体数：
  4
• 氢受体数：
  4

安全信息

• WGK Germany：
  3

反应信息

• 作为产物：
  描述：

  (+)-(6R)-2,6-二氨基-4,5,6,7-四氢苯并噻唑 、 4-甲基苯磺酸丙酯 在 4-甲基苯磺酸丙酯 作用下， 生成 R-普拉克索盐酸盐
  参考文献：
  名称：

  Tetrahedron Asymmetry 2014, 25, 1239-1245

  摘要：

  DOI：

文献信息

• MODIFICATIONS OF THERAPEUTIC AGENTS FOR ENHANCED DELIVERY TO TARGET SITES
  申请人：Partikula LLC

  公开号：US20180028647A1

  公开（公告）日：2018-02-01

  Compositions of a modulator of cell metabolism, typically targeting cellular glycolysis, preferably with a targeting moiety, attached directly or indirectly to the inhibitor, or to a nanoparticle or other delivery vehicle thereof, and methods of use for treating cancer, proliferative disorders, neurodegenerative diseases, autoimmune disorders, or inflammatory diseases are provided. Pharmaceutical compositions including the targeted modulator and a pharmaceutically acceptable carrier are also provided. The pharmaceutical compositions can be administered to a subject in need thereof in an effective amount to reduce one or symptoms of the cancer, proliferative disorders, neurodegenerative diseases, autoimmune disorders, or inflammatory diseases alone or prior to or in conjunction with a further therapy such as radiotherapy.

  提供了细胞代谢调节剂的组成，通常以靶向细胞糖酵解为目标，最好带有一个靶向基团，直接或间接连接到抑制剂，或连接到纳米颗粒或其他递送载体上，并提供了用于治疗癌症、增生性疾病、神经退行性疾病、自身免疫性疾病或炎症性疾病的方法。还提供了包括靶向调节剂和药学上可接受的载体的药物组合物。这些药物组合物可以以有效剂量给需要的受试者使用，以减少癌症、增生性疾病、神经退行性疾病、自身免疫性疾病或炎症性疾病的症状之一或多个，独立使用或在放疗等进一步治疗之前或同时使用。
• [EN] SYNTHESIS OF CHIRALLY PURIFIED SUBSTITUTED BENZOTHIAZOLE DIAMINES<br/>[FR] SYNTHÈSE DE BENZOTHIAZOLE-DIAMINES SUBSTITUÉES PURIFIÉES CHIRALEMENT
  申请人：KNOPP NEUROSCIENCES

  公开号：WO2011109596A1

  公开（公告）日：2011-09-09

  Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzotiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzotiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzotiazole diamines are provided herein.

  本文提供了制备手性纯净的取代4,5,6,7-四氢苯并噻唑二胺的方法，例如（6R）-2-氨基-4,5,6,7-四氢-6-(丙基氨基)苯并噻唑，并从手性富集的取代4,5,6,7-四氢苯并噻唑二胺混合物中提纯取代4,5,6,7-四氢苯并噻唑二胺的主对映体。
• DENDRIMER DELIVERY SYSTEM AND METHODS OF USE THEREOF
  申请人：The Johns Hopkins University

  公开号：US20190142964A1

  公开（公告）日：2019-05-16

  Low-generation dendrimers containing a high density of surface hydroxyl groups, and methods of synthesis thereof are provided. In particular, oligo ethylene glycol (OEG)-like dendrimers with a high surface functional groups at relatively low generations (e.g. ˜120 hydroxyls in the third generation, with a size of just 1-2 nm) is described. Dendrimer formulations including one or more prophylactic, therapeutic, and/or diagnostic agents, and methods of use thereof are also described. The formulations are suitable for topical, enteral, and/or parenteral delivery for treating one or more diseases, conditions, and injuries in the eye, the brain and nervous system (CNS), particularly those associated with pathological activation of microglia and astrocytes.

  本文提供了含有高密度表面羟基基团的低代数树状分子及其合成方法。具体来说，本文描述了具有高表面功能基团的寡聚乙二醇（OEG）类树状分子，其代数相对较低（例如第三代中约有120个羟基，大小仅为1-2纳米）。本文还描述了包括一种或多种预防性、治疗性和/或诊断性药物的树状分子制剂及其使用方法。这些制剂适用于局部、肠道和/或静脉注射治疗与微胶质细胞和星形胶质细胞病理激活相关的眼部、大脑和神经系统（CNS）中的一种或多种疾病、状况和损伤。
• [EN] IMPROVED SYNTHESIS OF AMINE SUBSTITUTED 4,5,6,7-TETRAHYDROBENZOTHIAZOLE COMPOUNDS<br/>[FR] SYNTHÈSE AMÉLIORÉE DE COMPOSÉS SUBSTITUÉS PAR AMINE DE 4,5,6,7-TÉTRAHYDROBENZOTHIAZOLE
  申请人：BIOGEN IDEC INC

  公开号：WO2013096816A1

  公开（公告）日：2013-06-27

  The present invention is related to an improved process for the preparation of amino- substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2- amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.

  本发明涉及一种改进的方法，用于制备公式I的氨基取代的4,5,6,7-四氢苯并噻唑化合物，例如化合物2-氨基-4,5,6,7-四氢-6-(n-丙基氨基)苯并噻唑。本发明还涉及(R)-2-氨基-4,5,6,7-四氢-6-(n-丙基氨基)苯并噻唑的改进合成方法。本发明还涉及与合成过程相关的方法和中间体。
• Synthesis of Chirally Purified Substituted Benzothiazole Diamines
  申请人：Greenfield Scott Jeffrey

  公开号：US20130079526A1

  公开（公告）日：2013-03-28

  Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro- 6 -(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein.

  本文提供了制备手性纯净的取代的4,5,6,7-四氢苯并噻唑二胺的方法，例如(6R)2-氨基-4,5,6,7-四氢-6-(丙基氨基)苯并噻唑，并从手性富集的混合物中纯化取代的4,5,6,7-四氢苯并噻唑二胺的优势对映体。