Fully automated synthesis module for the high yield one-pot preparation of 6-[ [formula omitted]]fluoro- l-DOPA
A fully automated one-pot synthesis of 6-[ 18 F ]fluoro- l-DOPA, an important radiopharmaceutical for studies on the presynaptic dopamine metabolism with positron emission tomography, is described. 6-[ 18 F ]Fluoro- l-DOPA was prepared in high radiochemical yield (33±4%, c.f.d.) and radiochemical pu...
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| Veröffentlicht in: | Applied radiation and isotopes 1999-10, Vol.51 (4), p.389-394 |
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| container_issue | 4 |
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| container_title | Applied radiation and isotopes |
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| creator | de Vries, Erik F.J Luurtsema, Gert Brüssermann, Michael Elsinga, Philip H Vaalburg, Willem |
| description | A fully automated one-pot synthesis of 6-[
18
F
]fluoro-
l-DOPA, an important radiopharmaceutical for studies on the presynaptic dopamine metabolism with positron emission tomography, is described. 6-[
18
F
]Fluoro-
l-DOPA was prepared in high radiochemical yield (33±4%, c.f.d.) and radiochemical purity (>99%) in 45 min synthesis time by a fluorodestannylation reaction, followed by acidic removal of the protecting groups. CFCl
3 was found to be a better solvent for the fluorodestannylation reaction than CHCl
3 or acetonitrile. In CFCl
3, [
18
F
]F
2 was a superior fluorinating agent over [
18
F
]acetyl hypofluorite. |
| doi_str_mv | 10.1016/S0969-8043(99)00057-3 |
| format | Article |
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18
F
]fluoro-
l-DOPA, an important radiopharmaceutical for studies on the presynaptic dopamine metabolism with positron emission tomography, is described. 6-[
18
F
]Fluoro-
l-DOPA was prepared in high radiochemical yield (33±4%, c.f.d.) and radiochemical purity (>99%) in 45 min synthesis time by a fluorodestannylation reaction, followed by acidic removal of the protecting groups. CFCl
3 was found to be a better solvent for the fluorodestannylation reaction than CHCl
3 or acetonitrile. In CFCl
3, [
18
F
]F
2 was a superior fluorinating agent over [
18
F
]acetyl hypofluorite.</description><identifier>ISSN: 0969-8043</identifier><identifier>EISSN: 1872-9800</identifier><identifier>DOI: 10.1016/S0969-8043(99)00057-3</identifier><language>eng</language><publisher>Elsevier Ltd</publisher><subject>Agents ; Drug products ; Fluorine compounds ; Metabolism ; Organic solvents ; Positron emission tomography</subject><ispartof>Applied radiation and isotopes, 1999-10, Vol.51 (4), p.389-394</ispartof><rights>1999 Elsevier Science Ltd</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c404t-4575a3419ef7a8356abc83864d6bdaefdc670b79219310d10aa23d03cb1b1573</citedby><cites>FETCH-LOGICAL-c404t-4575a3419ef7a8356abc83864d6bdaefdc670b79219310d10aa23d03cb1b1573</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0969804399000573$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids></links><search><creatorcontrib>de Vries, Erik F.J</creatorcontrib><creatorcontrib>Luurtsema, Gert</creatorcontrib><creatorcontrib>Brüssermann, Michael</creatorcontrib><creatorcontrib>Elsinga, Philip H</creatorcontrib><creatorcontrib>Vaalburg, Willem</creatorcontrib><title>Fully automated synthesis module for the high yield one-pot preparation of 6-[ [formula omitted]]fluoro- l-DOPA</title><title>Applied radiation and isotopes</title><description>A fully automated one-pot synthesis of 6-[
18
F
]fluoro-
l-DOPA, an important radiopharmaceutical for studies on the presynaptic dopamine metabolism with positron emission tomography, is described. 6-[
18
F
]Fluoro-
l-DOPA was prepared in high radiochemical yield (33±4%, c.f.d.) and radiochemical purity (>99%) in 45 min synthesis time by a fluorodestannylation reaction, followed by acidic removal of the protecting groups. CFCl
3 was found to be a better solvent for the fluorodestannylation reaction than CHCl
3 or acetonitrile. In CFCl
3, [
18
F
]F
2 was a superior fluorinating agent over [
18
F
]acetyl hypofluorite.</description><subject>Agents</subject><subject>Drug products</subject><subject>Fluorine compounds</subject><subject>Metabolism</subject><subject>Organic solvents</subject><subject>Positron emission tomography</subject><issn>0969-8043</issn><issn>1872-9800</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><recordid>eNqFkEtLxDAUhYMoOI7-BCEr0UU0afrKSsQ3CArObpCQJrdOJG1qkgrz7-044tbVhcN3DtwPoWNGzxll5cUrFaUgNc35qRBnlNKiInwHzVhdZUTUlO6i2R-yjw5i_JigvBbZDPm70bk1VmPynUpgcFz3aQXRRtx5MzrArQ94SvDKvq_w2oIz2PdABp_wEGBQQSXre-xbXJIlXk54NzqFfWfTtPf21rrRB0-wIzfPL1eHaK9VLsLR752jxd3t4vqBPD3fP15fPRGd0zyRvKgKxXMmoK1UzYtSNbrmdZmbsjEKWqPLijaVyJjgjBpGlcq4oVw3rGFFxefoZDs7BP85Qkyys1GDc6oHP0aZMV7VBd-AxRbUwccYoJVDsJ0Ka8mo3NiVP3blRp0UQv7YlXzqXW57MD3xZSHIqC30GowNoJM03v6z8A1L3YJ5</recordid><startdate>19991001</startdate><enddate>19991001</enddate><creator>de Vries, Erik F.J</creator><creator>Luurtsema, Gert</creator><creator>Brüssermann, Michael</creator><creator>Elsinga, Philip H</creator><creator>Vaalburg, Willem</creator><general>Elsevier Ltd</general><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>19991001</creationdate><title>Fully automated synthesis module for the high yield one-pot preparation of 6-[ [formula omitted]]fluoro- l-DOPA</title><author>de Vries, Erik F.J ; Luurtsema, Gert ; Brüssermann, Michael ; Elsinga, Philip H ; Vaalburg, Willem</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c404t-4575a3419ef7a8356abc83864d6bdaefdc670b79219310d10aa23d03cb1b1573</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Agents</topic><topic>Drug products</topic><topic>Fluorine compounds</topic><topic>Metabolism</topic><topic>Organic solvents</topic><topic>Positron emission tomography</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>de Vries, Erik F.J</creatorcontrib><creatorcontrib>Luurtsema, Gert</creatorcontrib><creatorcontrib>Brüssermann, Michael</creatorcontrib><creatorcontrib>Elsinga, Philip H</creatorcontrib><creatorcontrib>Vaalburg, Willem</creatorcontrib><collection>CrossRef</collection><jtitle>Applied radiation and isotopes</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>de Vries, Erik F.J</au><au>Luurtsema, Gert</au><au>Brüssermann, Michael</au><au>Elsinga, Philip H</au><au>Vaalburg, Willem</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Fully automated synthesis module for the high yield one-pot preparation of 6-[ [formula omitted]]fluoro- l-DOPA</atitle><jtitle>Applied radiation and isotopes</jtitle><date>1999-10-01</date><risdate>1999</risdate><volume>51</volume><issue>4</issue><spage>389</spage><epage>394</epage><pages>389-394</pages><issn>0969-8043</issn><eissn>1872-9800</eissn><abstract>A fully automated one-pot synthesis of 6-[
18
F
]fluoro-
l-DOPA, an important radiopharmaceutical for studies on the presynaptic dopamine metabolism with positron emission tomography, is described. 6-[
18
F
]Fluoro-
l-DOPA was prepared in high radiochemical yield (33±4%, c.f.d.) and radiochemical purity (>99%) in 45 min synthesis time by a fluorodestannylation reaction, followed by acidic removal of the protecting groups. CFCl
3 was found to be a better solvent for the fluorodestannylation reaction than CHCl
3 or acetonitrile. In CFCl
3, [
18
F
]F
2 was a superior fluorinating agent over [
18
F
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| fulltext | fulltext |
| identifier | ISSN: 0969-8043 |
| ispartof | Applied radiation and isotopes, 1999-10, Vol.51 (4), p.389-394 |
| issn | 0969-8043 1872-9800 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_21378537 |
| source | Elsevier ScienceDirect Journals Complete |
| subjects | Agents Drug products Fluorine compounds Metabolism Organic solvents Positron emission tomography |
| title | Fully automated synthesis module for the high yield one-pot preparation of 6-[ [formula omitted]]fluoro- l-DOPA |
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