Preparation Of N-monofluoroalkyl Tropanes


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.

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Document History
  • Publication: Jun 23, 2011
  • Application: Dec 15, 2010
    WO EP 2010069758 W
  • Priority: Dec 17, 2009
    GB GB 0922023 A
  • Priority: Dec 17, 2009
    US US 28726409 P

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