Parameter evaluation and fully-automated radiosynthesis of (11)Charmine for imaging of MAO-A for clinical trials.
The aim of the present study was the evaluation and automation of the radiosynthesis of (11)Charmine for clinical trials. The following parameters have been investigated amount of base, precursor concentration, solvent, reaction temperature and time. The optimum reaction conditions were determined to be 2-3mgmL precursor activated with 1eq. 5M NaOH in DMSO, 80°C reaction temperature and 2min reaction time. Under these conditions 6.1±1GBq (51.0±11% based on (11)CCH3I, corrected for decay) of (11)Charmine (n72) were obtained. The specific activity was 101.32±28.2GBqµmol (at EOS). All quality control parameters were in accordance with the standards for parenteral human application. Due to its reliability and high yields, this fully-automated synthesis method can be used as routine set-up.