Abstract A one-pot chemoselective bis (Suzuki–Miyaura cross-coupling) reaction under microwave irradiation is reported for the 4H-pyrido [1, 2-a] pyrimidin-4-one series. First, we ascertained an initial coupling reaction that was selectively carried out at the C-3 position of (7, 9-dichloro-3-iodo-4-oxo-4H-pyrido [1, 2-a] pyrimidin-2-yl) methyl acetate (4). Next, we developed an extremely efficient one-pot chemoselective bis (Suzuki–Miyaura cross- ...