carbovir | 118353-05-2

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 核苷和核苷酸类似物
• 英文名称: carbovir
• 英文别名: (9R)-2-amino-9-[(4S)-4-(hydroxymethyl)cyclopent-2-en-1-yl]purin-6-ol；2-amino-9-[(4S)-4-(hydroxymethyl)cyclopent-2-en-1-yl]-1H-purin-6-one
• CAS: 118353-05-2
• 化学式: C₁₁H₁₃N₅O₂
• 分子量: 247.257
• InChiKey: XSSYCIGJYCVRRK-ULUSZKPHSA-N

物化性质

• 熔点：
  267-269°C
• 沸点：
  390.29°C (rough estimate)
• 密度：
  1.2355 (rough estimate)
• 溶解度：
  可溶于二甲基亚砜、甲醇

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  106
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• PROCESS FOR THE PREPARATION OF AMINO ALCOHOL DERIVATIVES OR SALTS THEREOF
  申请人：GRANULES INDIA LIMITED

  公开号：US20170233329A1

  公开（公告）日：2017-08-17

  The present invention relates to a process for the preparation of amino alcohol derivatives or salts thereof. In particular the present invention relates to process for the preparation of amino alcohol derivatives or salts thereof which may be used as intermediates in the preparation of HIV reverse transcriptase inhibitors, more preferably Carbovir and Abacavir. The present invention more specifically relates to a process for the preparation of (1S,4R)-4-amino-2-cyclopentene-1-methanol of Formula IIIa. The present invention also specifically relates to process for the preparation of Abacavir sulfate of Formula II using compound of Formula IIIa prepared according to the process of the present invention.

  本发明涉及一种用于制备氨基醇衍生物或其盐的方法。特别是，本发明涉及一种用于制备氨基醇衍生物或其盐的方法，该方法可用作制备HIV逆转录酶抑制剂的中间体，更具体地是卡波韦和阿巴卡韦。本发明更具体地涉及一种用于制备Formula IIIa的(1S,4R)-4-氨基-2-环戊烯-1-甲醇的方法。本发明还具体涉及一种使用根据本发明方法制备的Formula IIIa化合物制备Formula II的阿巴卡韦硫酸盐的方法。
• Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
  申请人：Burnet Michael

  公开号：US20090093014A1

  公开（公告）日：2009-04-09

  This invention features a method of identifying a compound useful for enhancing efficacy of a therapeutic agent. The method includes incubating a compound in blood cells; separating immune cells from erythrocytic cells; and determining the ratio of the concentration of the compound in the immune cells to the concentration of the compound in the erythrocytic cells; wherein the compound comprises a transportophore and a therapeutic agent, in which the transportophore is covalently bonded to the therapeutic agent via a bond or a linker.

  这项发明涉及一种用于增强治疗剂效的化合物鉴定方法。该方法包括将化合物孵育在血细胞中；将免疫细胞与红细胞分离；并确定免疫细胞中化合物浓度与红细胞中化合物浓度之比；其中，该化合物包括一个运载体和一个治疗剂，其中运载体通过键合或连接物与治疗剂共价结合。
• Process for the preparation of amino alcohol derivatives or salts thereof
  申请人：GRANULES INDIA LIMITED

  公开号：US10385006B2

  公开（公告）日：2019-08-20

  The present invention relates to a process for the preparation of amino alcohol derivatives or salts thereof which may be used as intermediates in the preparation of HIV reverse transcriptase inhibitors, more preferably Carbovir and Abacavir. The present invention more specifically relates to a process for the preparation of (1S, 4R)-4-amino-2-cyclopentene-1-methanol of Formula IIIa.

  本发明涉及一种氨基醇衍生物或其盐的制备工艺，其可用作制备 HIV 逆转录酶抑制剂（更优选 Carbovir 和 Abacavir）的中间体。本发明更具体地涉及一种制备式 IIIa 的 (1S，4R)-4-氨基-2-环戊烯-1-甲醇的工艺。
• US7579324B2
  申请人：——

  公开号：US7579324B2

  公开（公告）日：2009-08-25
• US8357506B2
  申请人：——

  公开号：US8357506B2

  公开（公告）日：2013-01-22