(-)-2beta-Carbomethoxy-3beta-(4-iodophenyl)nortropane

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (-)-2beta-Carbomethoxy-3beta-(4-iodophenyl)nortropane
• 英文别名: methyl 3-(4-iodophenyl)-8-azabicyclo[3.2.1]octane-2-carboxylate
• 化学式: C₁₅H₁₈INO₂
• 分子量: 371.21
• InChiKey: IBOZZWGMZPMXBO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] PREPARATION OF N-MONOFLUOROALKYL TROPANES<br/>[FR] PRÉPARATION DE TROPANES N-MONOFLUOROALKYLÉS
  申请人：GE HEALTHCARE LTD

  公开号：WO2011073256A1

  公开（公告）日：2011-06-23

  The present invention relates to an improved synthesis of N-monofluoroalkyl tropanes using fluoroalkyl iodides or fluoroalkyl sulfonate esters. The invention also provides the use of such method to prepare the non-radioactive tropane intermediate FP-CIT, and its subsequent conversion to the 123I-labelled radiopharmaceutical DaTSCANTM (123I-ioflupane). Also provided is the use of fluoroalkyl iodides or fluoroalkyl sulfonate esters in the alkylation method of the invention.

  本发明涉及利用氟烷基碘化物或氟烷基磺酸酯改进合成N-单氟烷基托帕酮的方法。该发明还提供了利用这种方法制备非放射性托帕酮中间体FP-CIT，并将其进一步转化为123I标记的放射性药物DaTSCAN™（123I-ioflupane）的用途。该发明还提供了在本发明的烷基化方法中使用氟烷基碘化物或氟烷基磺酸酯的用途。
• PREPARATION OF N-MONOFLUOROALKYL TROPANES
  申请人：GE Healthcare Limited

  公开号：EP2513099B1

  公开（公告）日：2019-11-20
• METHOD FOR THE SYNTHESIS OF 18F-LABELLED BIOMOLECULES
  申请人：GE HEALTHCARE LIMITED

  公开号：US20140235861A1

  公开（公告）日：2014-08-21

  The present invention provides a method for the synthesis of 18 F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimised.
• METHOD FOR THE SYNTHESIS OF 18F-LABELLED MOLECULES
  申请人：GE HEALTHCARE LIMITED

  公开号：US20140243555A1

  公开（公告）日：2014-08-28

  The present invention provides a method for the synthesis of 18F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, in a preferred embodiment, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimised.
• PREPARATION OF N-MONOFLUOROALKYL COMPOUNDS
  申请人：GE Healthcare Limited

  公开号：US20160376265A1

  公开（公告）日：2016-12-29

  The present invention relates to an improved synthesis of N-monofluoroalkyl tropanes using fluoroalkyl iodide. The invention also provides the use of such method to prepare the non-radioactive tropane intermediate FP-CIT, and its subsequent conversion to the 123 I-labelled radiopharmaceutical DaTSCAN™ ( 123 I-ioflupane). Also provided is the use of fluoroalkyl iodide in the alkylation method of the invention.