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-lab...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: HAUGAN JARLE ANDRE, WILLIAMS LORENZO, KEILEN GUNNAR
Format: Patent
Sprache:chi ; eng
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Beschreibung
Zusammenfassung: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.