Solvent-free Synthesis of 5-Azacytosine with Microwave Activation

Azacytosine (4-amino-1,2-dihydro-1,3,5-triazin-2-one) is a very important intermediate in the synthesis of 5-azacytidine which showed remarkable bacteriostatic and cytostatic activity as well as against T-4 lymphoma and L-1210 leukemia in mice. Starting with N-cyanoguanidine (dicyandiamide) and formic acid, under the solvent-free microwave activation, we synthesized 5-azacytosine in short time (4min) with good yield (60.4%). The structure of the product was confirmed by HNMR and Elemental a…