PROCESS FOR PREPARING PYRIDO (2,3-D)PYRIMIDINE DERIVATIVES

摘要

Title compd. (I; R = pyrrolidino, 3-hydroxypyrrolidino, l-piperazinyl) was prepd. by 7 steps. N-amidinocyclic amino (II) was reacted with alkoxymethylene cyanoacetate(III) and then hydrolyzed and decarboxylated to give 2-cyclic amino-4-amino pyrimidine(IV). IV was reacted with alkoxymethylene malonate(v; R3 = lower alkyl)and then heated to give cyclic compd., which the H on 8-position was substituted by C2H5-followed by hydrolysis to give I.