SYNTHESIS AND ANTIVIRAL AND ANTITUMOR ACTIVITIES OF 2H-[1,2,3]TRIAZOLO[4,5-d]PYRIMIDINES AND 1H-,2H-,AND 3H-[1,2,3]TRIAZOLO[4,5-dPYRIMIDIN-5(4H)-ONE-7(6H)-THIONES

摘要

This paper describes a facile synthesis of 2-aryl-2H-[1,2,3]triazolo-[4,5-d]yrimidine-5,7(4H,6H)-diones (3a-o)and 7-amino-2-aryl-5-phenyl-2H-[l,2,3]triazolo[4,5-d]pyrimidines (6a-e)prepared by oxidative cyclization of 6-amino-5-arylazopyrimidine-2,4(lH,3H)-diones (2a-o)and 4,6-diamino-5-arylazo-2-phenylpyrimidines (5a-e)with CuSO_4,respectively,and a reliable thionation of [l,2,3]triazolo[4,5-d]pyrimidine-5,7(4H,6H)-diones (3a,e,f,7a,b and 9)accomplished by the reaction with phosphorous pentasulfide or Lawesson's reagent as well as evaluation of their antiviral and antitumor activities in vitro.