A no-carrier-added, high specific activity synthesis of [11C-methyl]-thymidine is reported. Reaction of 3′, 5′-O-bis-(tetrahydropyranyl)-5-bromo-2′-deoxyuridine with n-butyllithium produced a dianion which was alkylated with [11C]-methyl iodide, and on subsequent hydrolysis, yielded [11C-methyl]-thymidine. The labeled compound was isolated from the by-product 2′-deoxyuridine by HPLC on a reverse phase C18 semipreparative column with mean radiochemical yield of 18.8% (decay corrected) in 30-35 min and radiochemical purity >99%. This no-carrier-added synthesis can be used to produce [11C-methyl]-thymidine with mean specific activity over 1000 mCi/μmol for positron emission tomography (PET) studies.
ASJC Scopus subject areas
- Molecular Medicine
- Radiology Nuclear Medicine and imaging
- Cancer Research