Synthesis, quality control and tissue distribution of 2-[18F]-nicotinic acid diethylamide, a potential agent for regional cerebral function studies

Abstract

2-[18F]-nicotinic acid diethylamide was prepared by nucleophilic aromatic substitution in an acetamide melt of the corresponding chloro-compound and purified by high pressure liquid chromatography. Optimization of the reaction conditions led to a maximum radiochemical yield of about 50% within less than one half-life of18F. Tissue distribution of 2-[18F]-nicotinic acid diethylamide in various organs of mice showed a very fast accumulation of activity in the brain (mean body concentration MBC-239%) with a brain to blood ratio of 1.34.