Journal of labelled compounds and radiopharmaceuticals p. 1237 - 1246 (2006)
Update date:2022-08-11
Topics:
Kang, Se Han
Oh, Seung Jun
Yoon, Mi Kyung
Ryu, Jin Sook
Lee, Won Koo
Choi, Sun Joo
Park, Kyung Pae
Moon, Dae Hyuk
We synthesized 2'-deoxy-2'-[18F]fluorouridine (7) as a radiotracer for positron emission tomography from a new nosylate precursor (6). This new precursor was synthesized from uridine in four steps. The overall synthetic yield was 9.4 percent and we have high stability of >98 percent purity up to 6 months at 4 deg C. The optimal manual [18F]fluorination conditions were 30 mg of the precursor 6 in 500 μl of acetonitrile at 145 deg C for 15 min with 370 MBq of [18F]fluoride. The [18F]fluorination yield was 76.5 +/- 2.7 percent (n = 3). After hydrolysis of protecting groups with 1N HCl and purification by HPLC, the overall radiochemical yield and purity were 26.5 +/- 1.4 percent and 98.2 +/- 2.5 percent, respectively. The preparation time was 70.0 +/- 10.5 min (n = 3 for each result). We also developed an automated method with a radiochemical yield and purity of 24.0 +/- 2.8 and 98.0 +/- 1.5 percent (n = 10) using a GE TracerLab MX chemistry module. This new nosylate precursor for 2'-deoxy-2'-[18F]fluorouridine synthesis showed higher radiochemical yields and reproducibility than previous methods.
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