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À propos de : [11C]Carbon Monoxide in Selenium-Mediated Synthesis of11C-Carbamoyl Compounds        

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  • [11C]Carbon Monoxide in Selenium-Mediated Synthesis of11C-Carbamoyl Compounds
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  • Using either amines, amino alcohols, or alcohols in selenium-mediated synthesis with [11C]carbonmonoxide, 3 ureas, 6 carbamates, and 1 carbonate were labeled. Tetrabutylammonium fluoride((TBA)F) was discovered to form a soluble and reactive complex with selenium and drasticallyincrease the radiochemical yields. Of the selected carbamoyl compounds, one was a receptor ligand,one was an enzyme inhibitor, and one was a muscular relaxant pharmaceutical. The 11C-targetcompounds were obtained in radiochemical yields ranging from low to almost quantitative andwith specific radioactivity up to 1300 GBq/μmol. The radiochemical purity of the final productsexceeded 98%. In one case, the corresponding 13C-substituted compound was produced to verifythe position of the 11C-label. In a typical experiment starting with 16.4 GBq [11C]carbon monoxide,7.0 GBq of LC-purified 5-phenyl-1,3-oxazolidin-[2-11C]-2-one was obtained within 20 min from startof the carbonylation reaction (84% decay-corrected radiochemical yield). The presented approachis an interesting alternative to the use of [11C]phosgene in labeling chemistry.
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