氯沙坦三苯甲基醚 | 1006062-28-7

• 物质功能分类: 有机原料 - 醚类化合物及其衍生物
• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 中文名称: 氯沙坦三苯甲基醚
• 中文别名: 氯沙坦杂质I
• 英文名称: 5-(4'-((2-Butyl-4-chloro-5-(((triphenylmethyl)oxy)methyl)-1H-imidazol-1-yl)methyl)biphenyl-2-yl)-1H-tetrazole
• 英文别名: 5-[2-[4-[[2-butyl-4-chloro-5-(trityloxymethyl)imidazol-1-yl]methyl]phenyl]phenyl]-2H-tetrazole
• CAS: 1006062-28-7
• 化学式: C₄₁H₃₇ClN₆O
• 分子量: 665.2
• InChiKey: RIUQREUAFRCKLE-UHFFFAOYSA-N

物化性质

• 熔点：
  136-139?C
• 沸点：
  814.6±75.0 °C(Predicted)
• 密度：
  1.21±0.1 g/cm3(Predicted)
• 溶解度：
  可溶于氯仿（轻微）、DMSO、甲醇（轻微、加热、超声处理）

计算性质

• 辛醇/水分配系数(LogP)：
  9.5
• 重原子数：
  49
• 可旋转键数：
  13
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  81.5
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Crystalline form of losartan potassium
  申请人：DR. REDDY'S LABORATORIES LIMITED

  公开号：US20040097568A1

  公开（公告）日：2004-05-20

  A compound that is a crystalline Form III of losartan potassium is provided. Also provided are compositions containing the compound and methods for its preparation.

  提供了洛卡特普钾的结晶形式III的化合物。还提供了含有该化合物的组合物以及其制备方法。
• Process for the Preparation of Losartan
  申请人：Veera Reddy Arava

  公开号：US20100190996A1

  公开（公告）日：2010-07-29

  The invention relates to an improved process for the preparation of Losartan. The process comprising reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and an alkali, and reducing the resulting cyano aldehyde to produce a cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan.

  该发明涉及一种改进的洛卡特普制备过程。该过程包括在相转移催化剂和碱的存在下，将2-正丁基-4-氯-5-甲醛咪唑与2-(4-溴甲基)苯甲腈反应，然后还原生成的氰代醛以产生一种氰代醇，该氰代醇进一步与N-甲基吡咯烷酮和盐中的偶氮甲基钠反应以生成洛卡特普。
• Process for the preparation of losartan
  申请人：Veera Reddy Arava

  公开号：US20100222597A1

  公开（公告）日：2010-09-02

  The invention relates to a improved process for the preparation of Losartan and its potassium salt, which comprises: (i) reacting bromo OTBN with BCFI in the presence of a base and a phase transfer catalyst to produce a cyano aldehyde; reacting the formed cyano aldehyde with sodium azide in the presence of tributyl tin chloride to produce aldehyde tetrazole; reducing the formed aldehyde tetrazole with sodium borohydride to produce Losartan; and, if desired, converting the formed Losartan to its potassium salt by known method.

  这项发明涉及一种改进的制备洛卡特普及其钾盐的方法，包括：(i) 在碱和相转移催化剂的存在下，将溴代OTBN与BCFI反应以产生氰基醛；将形成的氰基醛与叠氮化钠在三丁基锡氯化物存在下反应以产生醛四唑；用硼氢化钠还原形成的醛四唑以产生洛卡特普；如有需要，通过已知方法将形成的洛卡特普转化为其钾盐。
• A process for the preparation of losartan derivatives by chlorination and reduction of the respective 1H-imidazole-5-carbaldehydes
  申请人：KRKA, D.D., Novo Mesto

  公开号：EP1741711A1

  公开（公告）日：2007-01-10

  The invention provides a process for the preparation of a sartan derivative of formula (I): wherein R = C2-C7 straight or branched alkyl or C3-C9 cycloalkyl, or a pharmaceutically acceptable salt thereof, comprising the steps of chlorinating and reducing, in any order, a compound of formula (III): wherein R is defined as above to form a compound of formula (VI), wherein R is defined as above and then deprotecting said compound of formula (VI) to obtain the sartan derivative of formula (I), and optionally converting said sartan derivative into one of its pharmaceutically acceptable salts. A preferred embodiment of this invention is a process for the preparation of losartan and, particularly, its potassium salt.

  本发明提供了一种制备公式（I）的萨替洛尔衍生物的过程：其中R = C2-C7直链或支链烷基或C3-C9环烷基，或其药学上可接受的盐，包括以下步骤：在任意顺序下进行氯化和还原，以形成公式（VI）的化合物，其中R如上所述，然后去保护该公式（VI）的化合物以获得公式（I）的萨替洛尔衍生物，并可选择将该萨替洛尔衍生物转化为其药学上可接受的盐之一。本发明的一种优选实施方案是制备洛卡新和特别是其钾盐的过程。
• Process for the synthesis of losartan potassium
  申请人：Kumar Ashok

  公开号：US20050070586A1

  公开（公告）日：2005-03-31

  Improved processes using primary, secondary and tertiary alcohols and with safer mode of introduction of the reagent and reaction conditions are described. Further, the process of manufacture of Losartan potassium by use of alkali metal salt such as Potassium carbonate is disclosed. A process for preparation of the polymorphic Form I of Losartan potassium is also disclosed herein.

  本文描述了使用一级、二级和三级醇改进的过程，并采用更安全的试剂引入和反应条件。此外，还公开了使用碱金属盐如碳酸钾制备洛卡特普钾的制造过程。本文还公开了制备洛卡特普钾多晶形式I的过程。