Source:http://linkedlifedata.com/resource/pubmed/id/18656910
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
16
|
pubmed:dateCreated |
2008-8-25
|
pubmed:abstractText |
An efficient and general method has been developed for fluorine-18 labeling of beta-blockers that possess the propanolamine moiety. A new synthetically versatile intermediate, 3-(1-(benzyloxy)propan-2-yl)-2-oxooxazolidin-5-yl)methyl 4-methylbenzenesulfonate (13), was prepared and can be conjugated to any phenoxy core. To demonstrate the synthetic methodology, fluorinated derivatives of toliprolol were prepared, namely, [(18)F]-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol ((2S and 2R)-[(18)F]1). The radiosyntheses were accomplished in <1 h, with 20-24% (uncorrected for decay, n = 7) radiochemical yields, >96% radiochemical and >99% enantiomeric purities, with specific activities of 0.9-1.1 Ci/micromol (EOS). Ex vivo biodistribution studies with the radiotracers demonstrated excessively rapid washout that may limit their use for cerebral PET imaging.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Aug
|
pubmed:issn |
1520-4804
|
pubmed:author | |
pubmed:issnType |
Electronic
|
pubmed:day |
28
|
pubmed:volume |
51
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
5093-100
|
pubmed:meshHeading |
pubmed-meshheading:18656910-Adrenergic beta-Antagonists,
pubmed-meshheading:18656910-Animals,
pubmed-meshheading:18656910-Brain,
pubmed-meshheading:18656910-Fluorine Radioisotopes,
pubmed-meshheading:18656910-Isotope Labeling,
pubmed-meshheading:18656910-Male,
pubmed-meshheading:18656910-Propanolamines,
pubmed-meshheading:18656910-Rats,
pubmed-meshheading:18656910-Rats, Sprague-Dawley
|
pubmed:year |
2008
|
pubmed:articleTitle |
Facile radiosynthesis of fluorine-18 labeled beta-blockers. Synthesis, radiolabeling, and ex vivo biodistribution of [18F]-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol.
|
pubmed:affiliation |
Centre for Addiction and Mental Health, 250 College Street, Toronto, Ontario, M5T 1R8 Canada.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|