Synthesis of ~(13)N-IabeIIed radiotracers by using microfluidic technology

摘要

Microfluidics has recently emerged as a useful alternative to traditional methods for the preparation of radiotracers labelled with positron emitters. Up to date, microfluidies technology has been applied to the radiosynthesis of ~(18)F-Iabelled and ~(11)C-labelied compounds; however, application to other shorter-lived positron emitters has not been investigated. The radiosynthesis of S-[~(13)N]nitrosothioIs and N-[~(13)N]nitrosamines was approached in microfluidic system by reaction of the corresponding thiol or secondary amine, respectively, with [~(13)N]NO_2~- in the presence of mineral acid. The radiosynthesis of azo compounds was carried out by reaction of the same labelling agent with primary aromatic amines in acidic media to yield the corresponding diazonium salts, which were further reacted with aromatic amines and alcohols to yield the corresponding ~(13)N-labelled azo compounds. Radiochemical conversion values for S-[~(13)N]nitrosothiols and ~(13)N-iabelled azo compounds calculated from chromatographic profiles improved our previous results by using conventional methods. The formation of N-[~(13)N]nitrosamines could not be detected, independently of experimental conditions. In conclusion, the preparation of S-[~(13)N]nitrosothiols and ~(13)N-Iabelled azo compounds was successfully achieved by using microfluidics technology. Higher radiochemicai conversions than those previously reported using conventional synthetic strategies have been obtained.