Reagents and conditions: (a)
dimethylphosphine oxide, Pd(OAc)2, xantphos, K3PO4, DMF, 120 °C, overnight, 82%; (b) R1 substituted pyrimidine, K2CO3, n-Bu4NHSO4, DMF, 65 °C, overnight, 63–84%;
(c) R2 substituted aniline, 2.5 M HCl in EtOH, 2-methoxyethanol,
120 °C, overnight, 37–75%.