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

摘要

There have been intensive studies concerning [11C]choline ([11C]methyldimethyl( モ-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 18F labelled choline (2) and proved to be useful to visualize prostate cancer. We have prepared six 18F 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 18F- in the presence of Kryptofix-2.2.2.. The labeling yields varied ranging from 7 to 25%.