A convenient two-step, one-pot synthesis of 4-chloro-2-(trichloromethyl)pyrimidines starting from 2-(trichloromethyl)-1,3-diazabutadienes is described. These nitrogen heterocycles were prepared by a sequential acylation/intramolecular cyclization reaction between 2-(trichloromethyl)-1,3-diazabutadienes and acyl chlorides in the presence of triethylamine followed by treatment with POCl3. This is the first report for the synthesis of this type of 4-chloro-2-(trichloromethyl)pyrimidine derivatives and serves as a source for a wide variety of other substituted pyrimidines by nucleophilic substitution reactions.
A one-pot synthesis of tetrasubstituted dihydropyrimidine and pyrimidine derivatives was developed on the basis of UV-LED photolysis of α-azidocinnamates as a key stage.
One-Pot Synthesis of Dihydro[1,2,4]triazolo[1,5-a]pyrimidines and Dihydrobenzo[4,5]imidazo[1,2-a]pyrimidine Derivatives Catalyzed by Amberlyst-15