A New and Facile Synthesis of 5-Arylpyrimidines and 4-Arylpyrazoles

A condensation of 2-aryl-3-(methy1thio)acrolelns (2) (21, a new masked form o f arylmalondialdehydes, wlth amidines yielded the corresponding 5-arylpyrlmidines (5)-(%I.Similarly, the reaction of 3 with N-substituted hydrazines gave the correspond .ing 1-substituted 4-arylpyrzolones (2) -(2).Considerable efforts have been directed toward the synthesis of a number of pyrimidine derivatives owing to their attractive biological ~mportance and many detailed reviews have appearedlv2.Of synthetic strategies, the condensation of 1,3-d~carbonyl compounds or thelr masked form with N -C -N fragments a r e known as the most w ~d e l y applicable method offering direct cntry into pyrimidine nucleus.3,4,5 Recently, a series of 5-aryl and 4-substituted 5-arylpyrimidine derivatives were appeared aimed at a synthesis of antiinflammatory active compounds by Sandoz group.h'e investigated a synthesis of a new masked form of arylmalondialdehydes,