Abstract：The 2-n-propylthio-4,6-dichloro-5-aminopyrimidine was used as raw material to synthesis the anticoagulant ticagrelor through a four-step reaction, including aromatic nucleophilic substitution, diazotization, aromatic nucleophilic substitution and deisopropylidene protection. In the first step of the aromatic nucleophilic substitution reaction, triethylamine and N,N-diisopropylethylamine system were used as the solvent and acid binding agent. The reaction time was greatly shortened, the conversion rate and yield were improved. In the third step of the aromatic nucleophilic substitution reaction, potassium carbonate was used as an acid binding agent, which simplified the post-processing and reduced environmental pollution. The synthetic method is simple to operate and easy to purify, and provides the possibility for industrial scale-up production.
