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 | Lorenzo Williams Jarle Andre Haugan Gunnar Keilen |
| 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.
La presente invención se refiere a una síntesis mejorada de N-monofluoroalquil tropanos utilizando yoduros fluoroalquilo o ésteres de fluoroalquil sulfonato. La presente invención también proporciona el uso de dicho método para preparar intermediarios de tropano no radioactivos FP-CIT, y su conversión posterior al DaTSCANTM (123l-yoflupano) radiofarmacéutico 123l-etiquetado. También se proporciona el uso de los yoduros fluroalquilo o los ésteres de sulfonato fluoroalquilo en el método de alquilación de la presente invención. |
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La presente invención se refiere a una síntesis mejorada de N-monofluoroalquil tropanos utilizando yoduros fluoroalquilo o ésteres de fluoroalquil sulfonato. La presente invención también proporciona el uso de dicho método para preparar intermediarios de tropano no radioactivos FP-CIT, y su conversión posterior al DaTSCANTM (123l-yoflupano) radiofarmacéutico 123l-etiquetado. También se proporciona el uso de los yoduros fluroalquilo o los ésteres de sulfonato fluoroalquilo en el método de alquilación de la presente invención.</description><language>eng ; spa</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM ; APPARATUS THEREFOR ; CHEMISTRY ; GENERAL METHODS OF ORGANIC CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>2016</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=20160603&DB=EPODOC&CC=MX&NR=339670B$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20160603&DB=EPODOC&CC=MX&NR=339670B$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>Lorenzo Williams</creatorcontrib><creatorcontrib>Jarle Andre Haugan</creatorcontrib><creatorcontrib>Gunnar Keilen</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.
La presente invención se refiere a una síntesis mejorada de N-monofluoroalquil tropanos utilizando yoduros fluoroalquilo o ésteres de fluoroalquil sulfonato. La presente invención también proporciona el uso de dicho método para preparar intermediarios de tropano no radioactivos FP-CIT, y su conversión posterior al DaTSCANTM (123l-yoflupano) radiofarmacéutico 123l-etiquetado. También se proporciona el uso de los yoduros fluroalquilo o los ésteres de sulfonato fluoroalquilo en el método de alquilación de la presente invención.</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</subject><subject>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</subject><subject>APPARATUS THEREFOR</subject><subject>CHEMISTRY</subject><subject>GENERAL METHODS OF ORGANIC CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2016</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZNAMCHINcAxyDPH091Pwd1Pw0_X19_N38wn1D_J39PGO9FEICfIPcPRzDeZhYE1LzClO5YXS3Axybq4hzh66qQX58anFBYnJqXmpJfG-EcbGlmbmBk7GBBUAAIjUI7o</recordid><startdate>20160603</startdate><enddate>20160603</enddate><creator>Lorenzo Williams</creator><creator>Jarle Andre Haugan</creator><creator>Gunnar Keilen</creator><scope>EVB</scope></search><sort><creationdate>20160603</creationdate><title>PREPARATION OF N-MONOFLUOROALKYL TROPANES</title><author>Lorenzo Williams ; Jarle Andre Haugan ; Gunnar Keilen</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_MX339670B3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; spa</language><creationdate>2016</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</topic><topic>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</topic><topic>APPARATUS THEREFOR</topic><topic>CHEMISTRY</topic><topic>GENERAL METHODS OF ORGANIC CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>Lorenzo Williams</creatorcontrib><creatorcontrib>Jarle Andre Haugan</creatorcontrib><creatorcontrib>Gunnar Keilen</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Lorenzo Williams</au><au>Jarle Andre Haugan</au><au>Gunnar Keilen</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PREPARATION OF N-MONOFLUOROALKYL TROPANES</title><date>2016-06-03</date><risdate>2016</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.
La presente invención se refiere a una síntesis mejorada de N-monofluoroalquil tropanos utilizando yoduros fluoroalquilo o ésteres de fluoroalquil sulfonato. La presente invención también proporciona el uso de dicho método para preparar intermediarios de tropano no radioactivos FP-CIT, y su conversión posterior al DaTSCANTM (123l-yoflupano) radiofarmacéutico 123l-etiquetado. También se proporciona el uso de los yoduros fluroalquilo o los ésteres de sulfonato fluoroalquilo en el método de alquilación de la presente invención.</abstract><oa>free_for_read</oa></addata></record> |
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| subjects | ACYCLIC OR CARBOCYCLIC COMPOUNDS ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM APPARATUS THEREFOR CHEMISTRY GENERAL METHODS OF ORGANIC CHEMISTRY HETEROCYCLIC COMPOUNDS METALLURGY ORGANIC CHEMISTRY |
| title | PREPARATION OF N-MONOFLUOROALKYL TROPANES |
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