An improved one-pot procedure for the preparation of [ 11C-carbonyl]-WAY100635
A simple one-pot procedure for the preparation of [ 11C-carbonyl]-WAY100635, a potent 5HT1A receptor antagonist, was developed. The procedure involves the trapping of 11CO 2 in a tetrahydrofuran (THF) solution of cyclohexylmagnesium chloride, elimination of excess Grignard reagents with anhydrous HC...
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| Veröffentlicht in: | Nuclear medicine and biology 1999-10, Vol.26 (7), p.815-819 |
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| creator | Hwang, Dah-Ren Simpson, Norman R Montoya, Julie Mann, J.John Laruelle, Marc |
| description | A simple one-pot procedure for the preparation of [
11C-carbonyl]-WAY100635, a potent 5HT1A receptor antagonist, was developed. The procedure involves the trapping of
11CO
2 in a tetrahydrofuran (THF) solution of cyclohexylmagnesium chloride, elimination of excess Grignard reagents with anhydrous HCl, reaction with SOCl
2, and the reaction of the resulting acid chloride with WAY100634 (2 mg) and triethylamine (20 μL) in THF. The total synthesis time is 45 min. Starting from 1326 ± 173 mCi of
11CO
2, the average amount of [
11C-carbonyl]-WAY100635 (
n
=40
) at end-of-synthesis (EOS) was 30 ± 13 mCi (2.3% radiochemical yield), or 148 ± 61 mCi (11%) at end-of-bombardment (EOB). The radiochemical purity was >99%, and the specific activity was 3.6 ± 1.9 Ci/μmol (EOS,
n
=40
), or 21.3 ± 9.8 Ci/μmol at EOB. This method is reliable and flexible for routine clinical studies. |
| doi_str_mv | 10.1016/S0969-8051(99)00056-6 |
| format | Article |
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11C-carbonyl]-WAY100635, a potent 5HT1A receptor antagonist, was developed. The procedure involves the trapping of
11CO
2 in a tetrahydrofuran (THF) solution of cyclohexylmagnesium chloride, elimination of excess Grignard reagents with anhydrous HCl, reaction with SOCl
2, and the reaction of the resulting acid chloride with WAY100634 (2 mg) and triethylamine (20 μL) in THF. The total synthesis time is 45 min. Starting from 1326 ± 173 mCi of
11CO
2, the average amount of [
11C-carbonyl]-WAY100635 (
n
=40
) at end-of-synthesis (EOS) was 30 ± 13 mCi (2.3% radiochemical yield), or 148 ± 61 mCi (11%) at end-of-bombardment (EOB). The radiochemical purity was >99%, and the specific activity was 3.6 ± 1.9 Ci/μmol (EOS,
n
=40
), or 21.3 ± 9.8 Ci/μmol at EOB. This method is reliable and flexible for routine clinical studies.</description><identifier>ISSN: 0969-8051</identifier><identifier>EISSN: 1872-9614</identifier><identifier>DOI: 10.1016/S0969-8051(99)00056-6</identifier><identifier>PMID: 10628562</identifier><language>eng</language><publisher>Amsterdam: Elsevier Inc</publisher><subject>5HT1A receptor ; Antagonist ; Biological and medical sciences ; Carbon Dioxide - chemistry ; Carbon Radioisotopes ; Carbon-11 ; Contrast media. Radiopharmaceuticals ; Furans - chemistry ; Investigative techniques, diagnostic techniques (general aspects) ; Isotope Labeling - instrumentation ; Isotope Labeling - methods ; Medical sciences ; Nervous system ; PET ; Pharmacology. Drug treatments ; Piperazines - chemical synthesis ; Pyridines - chemical synthesis ; Radiochemistry ; Radionuclide investigations ; Radiopharmaceuticals - chemical synthesis ; Serotonin Antagonists - chemical synthesis ; WAY100635</subject><ispartof>Nuclear medicine and biology, 1999-10, Vol.26 (7), p.815-819</ispartof><rights>1999 Elsevier Science Inc.</rights><rights>2000 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c437t-58be2c8200b051b76c64619b647f441aefa7c63f9415f4e152230395a18efac63</citedby><cites>FETCH-LOGICAL-c437t-58be2c8200b051b76c64619b647f441aefa7c63f9415f4e152230395a18efac63</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0969-8051(99)00056-6$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27929,27930,46000</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1237746$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10628562$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Hwang, Dah-Ren</creatorcontrib><creatorcontrib>Simpson, Norman R</creatorcontrib><creatorcontrib>Montoya, Julie</creatorcontrib><creatorcontrib>Mann, J.John</creatorcontrib><creatorcontrib>Laruelle, Marc</creatorcontrib><title>An improved one-pot procedure for the preparation of [ 11C-carbonyl]-WAY100635</title><title>Nuclear medicine and biology</title><addtitle>Nucl Med Biol</addtitle><description>A simple one-pot procedure for the preparation of [
11C-carbonyl]-WAY100635, a potent 5HT1A receptor antagonist, was developed. The procedure involves the trapping of
11CO
2 in a tetrahydrofuran (THF) solution of cyclohexylmagnesium chloride, elimination of excess Grignard reagents with anhydrous HCl, reaction with SOCl
2, and the reaction of the resulting acid chloride with WAY100634 (2 mg) and triethylamine (20 μL) in THF. The total synthesis time is 45 min. Starting from 1326 ± 173 mCi of
11CO
2, the average amount of [
11C-carbonyl]-WAY100635 (
n
=40
) at end-of-synthesis (EOS) was 30 ± 13 mCi (2.3% radiochemical yield), or 148 ± 61 mCi (11%) at end-of-bombardment (EOB). The radiochemical purity was >99%, and the specific activity was 3.6 ± 1.9 Ci/μmol (EOS,
n
=40
), or 21.3 ± 9.8 Ci/μmol at EOB. This method is reliable and flexible for routine clinical studies.</description><subject>5HT1A receptor</subject><subject>Antagonist</subject><subject>Biological and medical sciences</subject><subject>Carbon Dioxide - chemistry</subject><subject>Carbon Radioisotopes</subject><subject>Carbon-11</subject><subject>Contrast media. Radiopharmaceuticals</subject><subject>Furans - chemistry</subject><subject>Investigative techniques, diagnostic techniques (general aspects)</subject><subject>Isotope Labeling - instrumentation</subject><subject>Isotope Labeling - methods</subject><subject>Medical sciences</subject><subject>Nervous system</subject><subject>PET</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperazines - chemical synthesis</subject><subject>Pyridines - chemical synthesis</subject><subject>Radiochemistry</subject><subject>Radionuclide investigations</subject><subject>Radiopharmaceuticals - chemical synthesis</subject><subject>Serotonin Antagonists - chemical synthesis</subject><subject>WAY100635</subject><issn>0969-8051</issn><issn>1872-9614</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkMFKJDEQhoMoOqs-gtIHkd1DNNWdpDsnGQZ1BdGDuyyLSEhnKhjp6YxJj-Dbm3EG9eYpVOqrqp-PkANgJ8BAnt4xJRVtmICfSv1ijAlJ5QYZQVOXVEngm2T0geyQHyk9sTzHgW2THWCybIQsR-Rm3Bd-No_hBadF6JHOw1Dk0uJ0EbFwIRbDI-YfnJtoBh_6IrjivgCYUGtiG_rX7oH-G_8HxmQl9siWM13C_fW7S_5enP-Z_KbXt5dXk_E1tbyqByqaFkvblIy1OV1bSyu5BNVKXjvOwaAztZWVUxyE4wiiLCtWKWGgya3c2SXHq7056vMC06BnPlnsOtNjWCQtVaWykyaDYgXaGFKK6PQ8-pmJrxqYXorU7yL10pJWSr-L1MsDh-sDi3aG0y9TK3MZOFoDJlnTuWh669MnV1Z1zZd7zlYYZhsvHqNO1mOf9fqIdtDT4L9J8gbAG4xx</recordid><startdate>19991001</startdate><enddate>19991001</enddate><creator>Hwang, Dah-Ren</creator><creator>Simpson, Norman R</creator><creator>Montoya, Julie</creator><creator>Mann, J.John</creator><creator>Laruelle, Marc</creator><general>Elsevier Inc</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19991001</creationdate><title>An improved one-pot procedure for the preparation of [ 11C-carbonyl]-WAY100635</title><author>Hwang, Dah-Ren ; Simpson, Norman R ; Montoya, Julie ; Mann, J.John ; Laruelle, Marc</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c437t-58be2c8200b051b76c64619b647f441aefa7c63f9415f4e152230395a18efac63</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>5HT1A receptor</topic><topic>Antagonist</topic><topic>Biological and medical sciences</topic><topic>Carbon Dioxide - chemistry</topic><topic>Carbon Radioisotopes</topic><topic>Carbon-11</topic><topic>Contrast media. Radiopharmaceuticals</topic><topic>Furans - chemistry</topic><topic>Investigative techniques, diagnostic techniques (general aspects)</topic><topic>Isotope Labeling - instrumentation</topic><topic>Isotope Labeling - methods</topic><topic>Medical sciences</topic><topic>Nervous system</topic><topic>PET</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperazines - chemical synthesis</topic><topic>Pyridines - chemical synthesis</topic><topic>Radiochemistry</topic><topic>Radionuclide investigations</topic><topic>Radiopharmaceuticals - chemical synthesis</topic><topic>Serotonin Antagonists - chemical synthesis</topic><topic>WAY100635</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hwang, Dah-Ren</creatorcontrib><creatorcontrib>Simpson, Norman R</creatorcontrib><creatorcontrib>Montoya, Julie</creatorcontrib><creatorcontrib>Mann, J.John</creatorcontrib><creatorcontrib>Laruelle, Marc</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Nuclear medicine and biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Hwang, Dah-Ren</au><au>Simpson, Norman R</au><au>Montoya, Julie</au><au>Mann, J.John</au><au>Laruelle, Marc</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>An improved one-pot procedure for the preparation of [ 11C-carbonyl]-WAY100635</atitle><jtitle>Nuclear medicine and biology</jtitle><addtitle>Nucl Med Biol</addtitle><date>1999-10-01</date><risdate>1999</risdate><volume>26</volume><issue>7</issue><spage>815</spage><epage>819</epage><pages>815-819</pages><issn>0969-8051</issn><eissn>1872-9614</eissn><abstract>A simple one-pot procedure for the preparation of [
11C-carbonyl]-WAY100635, a potent 5HT1A receptor antagonist, was developed. The procedure involves the trapping of
11CO
2 in a tetrahydrofuran (THF) solution of cyclohexylmagnesium chloride, elimination of excess Grignard reagents with anhydrous HCl, reaction with SOCl
2, and the reaction of the resulting acid chloride with WAY100634 (2 mg) and triethylamine (20 μL) in THF. The total synthesis time is 45 min. Starting from 1326 ± 173 mCi of
11CO
2, the average amount of [
11C-carbonyl]-WAY100635 (
n
=40
) at end-of-synthesis (EOS) was 30 ± 13 mCi (2.3% radiochemical yield), or 148 ± 61 mCi (11%) at end-of-bombardment (EOB). The radiochemical purity was >99%, and the specific activity was 3.6 ± 1.9 Ci/μmol (EOS,
n
=40
), or 21.3 ± 9.8 Ci/μmol at EOB. This method is reliable and flexible for routine clinical studies.</abstract><cop>Amsterdam</cop><pub>Elsevier Inc</pub><pmid>10628562</pmid><doi>10.1016/S0969-8051(99)00056-6</doi><tpages>5</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0969-8051 |
| ispartof | Nuclear medicine and biology, 1999-10, Vol.26 (7), p.815-819 |
| issn | 0969-8051 1872-9614 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_69390008 |
| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | 5HT1A receptor Antagonist Biological and medical sciences Carbon Dioxide - chemistry Carbon Radioisotopes Carbon-11 Contrast media. Radiopharmaceuticals Furans - chemistry Investigative techniques, diagnostic techniques (general aspects) Isotope Labeling - instrumentation Isotope Labeling - methods Medical sciences Nervous system PET Pharmacology. Drug treatments Piperazines - chemical synthesis Pyridines - chemical synthesis Radiochemistry Radionuclide investigations Radiopharmaceuticals - chemical synthesis Serotonin Antagonists - chemical synthesis WAY100635 |
| title | An improved one-pot procedure for the preparation of [ 11C-carbonyl]-WAY100635 |
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