反应详情

温度

120 °C

K2CO3 (60.3 mg, 0.436 mmol) and bis(triphenylphosphine) palladium(II) dichloride (10.21 mg, 0.015 mmol) were each rapidly added in sequence to a suspension of 7-chloro-5-methyl-2-(2-[1,2,4]triazolo[1,5-a]pyridin-2-yl-ethyl)-3,5-dihydro-2H-pyrrolo[3,4-c]pyridine-1,6-dione (50 mg, 0.145 mmol, see Example c6)) and pyridin-3-ylboronic acid (19.67 mg, 0.160 mmol) in DMF (1 ml)/water (0.200 ml). The reaction mixture was heated in a microwave at about 120° C. for about 20 min. The mixture was purified by preparative HPLC (system: Waters 2767 PHW003, eluent: MeCN/ammonium acetate buffer (gradient: 5:95 to 30:70 over 15 min), column: Boston Analytics, C-18, 10 μm, 21×250 mm) to afford the title compound (25 mg, 0.065 mmol, 44.5% yield).

1. customThe mixture was purified by preparative HPLC (system: Waters 2767 PHW003, eluent: MeCN/ammonium acetate buffer (gradient: 5:95 to 30:70 over 15 min), column: Boston Analytics, C-18, 10 μm, 21×250 mm)