In order to find more activity antitumor PI3K inhibitors, pyrimidine-2,4-diol as raw material, after chlorinated by POCl3, coupled with morpholine, then lodine generation, followed with Sonogashira coupling and remove the trimethylsilyl to get the triazolyl intermediate, finally, Suzuki coupling to get 2-aryl-4-morpholino-6-triazolylpyrimidine 14~27, their structures were confirmed by 1H NMR and LC-MS. The in vitro anti-proliferative activity assay against A2780 has been cacacarried out by MTT detection method, the result showed that under the test concentration of 10 μmol L-1, the compounds 14 and 25 were more potent than clinical candidates GDC-0941 and BEZ-235, inhibition rate reached 76.7%, 77.2% respectively. Furthermore, the result of pharmacokinetic study suggested that compounds 25 was desirable.t1/2=3.2 h, AUC0-∞ was 34193 ng•h•mL-1.