Synthesis of[~(18)F]Fluorocholine Analogues as a Potential Imaging Agent for PET Studies

摘要

There have been intensive studies concerning[~(11)'C]choline([~(11)C]methyldimethyl(beta-hydroxyethyl)ammonium)(1)which is known as a very effective tracer in imaging various human tumors localized in brain,lung,esophagus,rectum,prostate and urinary bladder using Positron Emission Tomography(PET)and there is increasing interest in ~(18)F labelled choline(2)and proved to be useful to visualize prostate cancer.We have prepared six ~(18)F labelled alkyl choline derivatives(3a-3c,4a-4c)from ditosylated and dibrominated alkanes in moderate yields.The six alkyl tosylate or bromate ammonium salts have been synthesized as precursors.Radiofluorination was achieved by the treatment of precursors with ~(18)F~- in the presence of Kryptofix-2.2.2..The labeling yields varied ranging from 7 to 25%.