AZETIDINIUM SALT AS FP-CIT PRECURSOR, SELECTIVE PREPARATION METHOD THEREOF, AND SYNTHESIS OF FP-CIT

摘要

PURPOSE: An azetidium salt of N-(3-sulfonyloxypropyl)-2-b-carbomethoxy-3-b-(4-iodophenyl)trophane compound is provided to be used as a precursor for preparing [18F]FP-CIT. CONSTITUTION: An azetidium salt is denoted by chemical formula 1(1'R,2'S,3'S,5'S)-3'-(4-iodophenyl)-2'-(methoxycarbonyl)spiro[azetidine-1,8'-bicylo[3.2.1]octane]-1-yum R-substituted sulfonate). A method for selectively preparing a compound of chemical formula 1 comprises a step of using polar solvent with 0.38 or more of ETN(normalized standard solvent polarity) level from a compound of chemical formula 2. The polar solvent is dimethyl formamide, t-butanol, acetonitrile, methanol, ethanol, isopropanol, dimethyl sulfoxide, t-amyl alcohol or water.