93319-46-1

This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X1, X2, X3, X4 are, independently at each occurrence, C, O, S, Se, N and P elements; R1, R2, R3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.

Catalytic hydrogenation of 3-(2-aminoaryl)-1,2,4-oxadiazoles (9, 12, 15, 18, 21) to 2-amino-N-acylarenecarboxamidines (10, 13, 16, 19, 22) followed by dehydration gave condensed 4-amino-pyrimidines (11, 14, 17, 20, 23), while the corresponding secondary amines (24) afforded 1,2-disubstituted 4-iminoquinazolines (26).Reduction and dehydration of 3--1,2,4-oxadiazoles (28) provided, via a somewhat different pathway, 4-(acylamino)quinazolines (31).