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...
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| 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.
Cette invention concerne un procédé de synthèse amélioré de tropanes N-monofluoroalkylés à partir d'iodures de fluoroalkyle ou d'esters de sulfonates fluoroalkylés. L'invention concerne également l'utilisation de ce procédé pour préparer l'intermédiaire de tropane non radioactif, FP-CIT, et sa conversion ultérieure en DaTSCANTM radiopharmaceutique marqué au 123I (ioflupane 123I). L'utilisation des iodures de fluoroalkyle ou des esters de sulfonates fluoroalkylés dans le procédé d'alkylation selon l'invention est également décrite. |
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