[(1S)-4-(2-amino-6-chloropurin-9-yl)cyclopent-2-en-1-yl]methanol

• 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: [(1S)-4-(2-amino-6-chloropurin-9-yl)cyclopent-2-en-1-yl]methanol
• 化学式: C₁₁H₁₂ClN₅O
• 分子量: 265.7
• InChiKey: IHEDZPMXLKYPSA-ULUSZKPHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 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：
  89.8
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• PROCESS FOR THE PREPARATION OF AMINOALCOHOL DERIVATIVES AND THEIR FURTHER CONVERSION TO (1R, 4S)-4(2-AMINO-6-CHLORO-5-FORMAMIDO-4- PYRIMIDINYL)-AMINO-2-CYCLOPENTENYL-1-METHANOL
  申请人：Brieden Walter

  公开号：US20070123545A1

  公开（公告）日：2007-05-31

  The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl)formamide of the formula to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.

  本发明涉及一种新的制备式为2-azabicyclo[2.2.1]庚-5-烯-3-酮的氨基醇的方法，该氨基醇可以是外消旋或光学活性的，进一步转化为相应的酰基衍生物，然后进一步转化为式为(1S,4R)-或(1R,4S)-4-(2-氨基-6-氯-9-H-嘌呤-9-基)-2-环戊烯基-1-甲醇的化合物。在后一种合成中，氨基醇被转化为相应的D-或L-酒石酸盐，然后与式为N-(2-氨基-4,6-二氯嘧啶-5-基)甲酰胺的化合物反应，得到式为(1S,4R)-或(1R,4S)-4-[(2-氨基-6-氯-5-甲酰胺基-4-嘧啶基)氨基]-2-环戊烯基-1-甲醇的化合物，然后环化得到最终产物。
• PROCESS FOR THE PREPARATION OF (1S,4R)-CIS-4-[2-AMINO-6-CHLORO-9H-PURIN-9-YL]-2-CYCLOPENTENE-1-METHANOL
  申请人：GLAXO GROUP LIMITED

  公开号：EP1660498B1

  公开（公告）日：2007-08-22
• EP1982985A2
  申请人：——

  公开号：EP1982985A2

  公开（公告）日：2008-10-22
• Process for the preparation of (1s, 4r)-cis-4-'2-amino-6chloro-9h-purin-yl!-2-cyclopentene-1- methanol
  申请人：Lawrence Maxwell Ronnie

  公开号：US20070027316A1

  公开（公告）日：2007-02-01

  The present invention relates to a process for preparing a chloropurine compound of formula (I)
• ANTIVIRAL 4-(2-AMINO-6-HETEROCYLYL-9H-PURIN-9-YL)-2-CYCLOPENTENE-1 -METHANOL COMPOUNDS
  申请人：THE UNIVERSITY OF LIVERPOOL

  公开号：US20190000853A1

  公开（公告）日：2019-01-03

  The present invention relates to certain antiviral compounds of formula I as defined herein that function as nucleoside reverse transcriptase inhibitors. The present invention also relates to processes for the preparation of these compounds, pharmaceutical compositions comprising them and to their use for the treatment of retroviral infections, and in particular their use in the treatment of HIV-1 virus.