High radiochemical yield synthesis of 3′-deoxy-3′-[18F]fluorothymidine using (5′-O-dimethoxytrityl-2′-deoxy-3′-O-nosyl-β-D-threo pentofuranosyl)thymine and its 3-N-BOC-protected analogue as a labeling precursor

Add time:08/18/2019    Source:sciencedirect.com

We prepared 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT) from 3′-O-nosyl thymidine derivative 3 or its pyrimidine ring N-BOC-protected analogue 5 and optimized [18F]fluorination condition for a high radiochemical yield. The optimal condition for [18F]fluorination with precursor 3 was 30 mg (41.1 μmol)/300 μl CH3CN at 130°C for 5 min, while precursor 5 required 34 mg (40 μmol)/300 μl CH3CN at 110°C for 5 min. After HPLC purification at neutral pH, we achieved high radiochemical yields of 40 ± 5.2% and 42 ± 5.4% (decay-corrected) within 60 min of preparation time with radiochemical purities of >97%.

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