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Z. Naturforsch. 2012, 67b, 827 – 834
doi:10.5560/ZNB.2012-0047
Synthesis and Biological Evaluation of 7-(2-Chlorophenylamino)-5-((2-[18F]fluoro-ethyoxy)methyl)pyrazolo[1,5-a]pyrimidine-3-carbonitrile as PET Tumor Imaging Agent
Jingli Xu, Hang Liu, Guixia Li, Yong He, Rui Ding, Xiao Wang, Man Feng, Shuting Zhang, Yurong Chen, Shilei Li, Mingxia Zhao, Yingruo Li, and Chuanmin Qi
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China
Reprint requests to Prof. C. M. Qi. E-mail: qicmin@sohu.com
Received February 10, 2012 / published online August 20, 2012
An 18F-labeled pyrazolo[1,5-a]pyrimidine derivative, 7-(2-chlorophenylamino)-5-((2-[18F]fluoroethyoxy)methyl)pyrazolo[1,5-a]pyrimidine-3-carbonitrile ([18F]5), has been designed and prepared as a radio tracer candidate for tumor detection with positron emission tomography (PET). The desired product [18F]5 was synthesized by nucleophilic substitution of the corresponding tosylated precursor with [18F]KF/Kryptofix 2.2.2 and potassium carbonate in anhydrous DMF at 100 °C for 20 min followed by purification with HPLC. The radiochemical purity was > 98 %, and the radio-chemical yield was 25 % (decay-uncorrected). Compound [18F]5 was very stable in vitro. The biodistribution study in mice bearing S180 tumors demonstrated that [18F]5 had a rapid and prolonged accumulation in tumors with moderate washout from other tissues.
Key words: Pyrazolo[1,5-a]pyrimidine Derivative, 7-(2-Chlorophenylamino)-5-((2-[18F]fluoroethyoxy)methyl)pyrazolo[1,5-a]pyrimidine-3-carbonitrile, Radiotracer, Tumor Detection, Positron Emission Tomography
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