RTI-55

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 托烷生物碱
• 英文名称: RTI-55
• 英文别名: 3-(4-Iodo-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester；methyl 3-(4-iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
• 化学式: C₁₆H₂₀INO₂
• 分子量: 385.245
• InChiKey: SIIICDNNMDMWCI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  methyl 8-methyl-3-phenyl-8-azabicyclo[3.2.1]octane-4-carboxylate 在 碘 、 silver trifluoromethanesulfonate 作用下， 以 二氯甲烷 为溶剂， 以88%的产率得到RTI-55
  参考文献：
  名称：

  A DIRECT IODINATION METHOD WITH IODINE AND SILVER TRIFLATE FOR THE SYNTHESIS OF SPECT AND PET IMAGING AGENT PRECURSORS

  摘要：

  A direct iodination method with iodine and silver triflate for the synthesis of SPECT and PET imaging agent precursors has been developed.

  DOI：

  10.1081/scc-100105877

文献信息

• [EN] METHOD FOR THE SYNTHESIS OF 18F-LABELLED BIOMOLECULES<br/>[FR] PROCÉDÉ DE SYNTHÈSE DE BIOMOLÉCULES MARQUÉES AU 18F
  申请人：GE HEALTHCARE LTD

  公开号：WO2013053941A1

  公开（公告）日：2013-04-18

  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.

  本发明提供一种合成18F标记生物分子的方法，适用于自动化。本发明还提供一种用于自动化本发明方法的盒子。与现有技术相比，本发明方法提供了许多优点。与已知方法相比，只需要少一步纯化。此外，在优选实施例中，只需要少一种试剂，因为一种特定试剂在两个不同的步骤中被使用。化学过程因此变得简化，商品成本降低，对于GMP临床生产所需试剂的验证和文档记录的负担也减少了。
• CHEMICAL SYNTHESIS OF I-124BETA CIT IODINE-124 [2-BETA-CARBOMETHOXY-3BETA- (4. -IODOPHENYL) -TROPANE] FOR PET INVESTIGATIONS AND FOR RADIOTHERAPY
  申请人：A.C.O.M. Advanced Center Oncology Macerata S.p.a.

  公开号：EP2212320A1

  公开（公告）日：2010-08-04
• METHOD FOR THE SYNTHESIS OF 18F-LABELLED BIOMOLECULES
  申请人：GE Healthcare Limited

  公开号：EP2766325A1

  公开（公告）日：2014-08-20
• PREPARATION OF N-MONOFLUOROALKYL COMPOUNDS
  申请人：GE Healthcare Limited

  公开号：US20220009919A1

  公开（公告）日：2022-01-13

  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.
• US6344179B1
  申请人：——

  公开号：US6344179B1

  公开（公告）日：2002-02-05