Synthesis Precursor of Apoptosis Imaging Agent ¹⁸F-ML-10 and Its Radiolabing With ¹⁸F

¹⁸F-2-(5-fluoro-pentyl)-2-methyl malonic acid(¹⁸F-ML-10) is one of the competitive candidate for apoptosis imaging with PET. ML-10 as reference and its OTs derivative (diethyl 2-methyl-2-(5-(tosyloxy)pentyl) malonate) as precursor for labeling with fluorine-18 were prepared. ¹⁸F-ML-10 was synthesized via nucleophilic substitution and base hydrolysis. The ¹⁸F-ML-10 injection was got by semi-HPLC and solid-extraction-preparation via home MF-2V-IT-1 module. The synthesis yield of ¹⁸F-ML-10 is （25.3±4.7）%（n=16, no corrected decay）, and the specific activity is 740 PBq/mol. The radiochemical purity is over 99%. The residuary acetonitrile in the injection is (0.015±0.01)%（w）. The K2.2.2 mass concentration in the injection is low than 10 mg/L. The injection is free of bacteria and pyrogen. It can be used for clinical research.