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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| creator | WILLIAMS, LORENZO KEILEN, GUNNAR HAUGAN, JARLE ANDRE |
| description | 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. |
| format | Patent |
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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.</description><language>eng ; fre</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>2011</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20110623&DB=EPODOC&CC=WO&NR=2011073256A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,777,882,25545,76296</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20110623&DB=EPODOC&CC=WO&NR=2011073256A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>WILLIAMS, LORENZO</creatorcontrib><creatorcontrib>KEILEN, GUNNAR</creatorcontrib><creatorcontrib>HAUGAN, JARLE ANDRE</creatorcontrib><title>PREPARATION OF N-MONOFLUOROALKYL TROPANES</title><description>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.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2011</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZNAMCHINcAxyDPH091Pwd1Pw0_X19_N38wn1D_J39PGO9FEICfIPcPRzDeZhYE1LzClO5YXS3AzKbq4hzh66qQX58anFBYnJqXmpJfHh_kYGhoYG5sZGpmaOhsbEqQIA5x0lpA</recordid><startdate>20110623</startdate><enddate>20110623</enddate><creator>WILLIAMS, LORENZO</creator><creator>KEILEN, GUNNAR</creator><creator>HAUGAN, JARLE ANDRE</creator><scope>EVB</scope></search><sort><creationdate>20110623</creationdate><title>PREPARATION OF N-MONOFLUOROALKYL TROPANES</title><author>WILLIAMS, LORENZO ; KEILEN, GUNNAR ; HAUGAN, JARLE ANDRE</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_WO2011073256A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fre</language><creationdate>2011</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>WILLIAMS, LORENZO</creatorcontrib><creatorcontrib>KEILEN, GUNNAR</creatorcontrib><creatorcontrib>HAUGAN, JARLE ANDRE</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>WILLIAMS, LORENZO</au><au>KEILEN, GUNNAR</au><au>HAUGAN, JARLE ANDRE</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PREPARATION OF N-MONOFLUOROALKYL TROPANES</title><date>2011-06-23</date><risdate>2011</risdate><abstract>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.</abstract><oa>free_for_read</oa></addata></record> |
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| title | PREPARATION OF N-MONOFLUOROALKYL TROPANES |
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