SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINES

novel substituted pyrimidines were synthesized from methyl 2,4-dioxo-4-phenyl-butanoate (i-a) and urea, followed by mitsunobu coupling of i-a with benzyl or allyl alcohol to give the corresponding 2-hydroxypyrimidine ethers in good yields. saponification of i-a, followed by reaction with benzyl or allyl amines in the presence of tbtu yielded 2-hydroxy-6-phenyl-pyrimidine 4-carboxamides. ache and buche assays revealed 2-hydroxy-6-phenyl-pyrimidine-4-carboxyallyamide as the most active compound, ic50= 90 μm, with no inhibition of buche.