Water → 5-Methyl-2-[2-(1-methyl-1H-benzoimidazol-2-yl)-ethyl]-7-pyridin-3-yl-3,5-dihydro-2H-pyrrolo[3,4-c]pyridine-1,6-dione

Participants

Reaction Conditions

Reaction Steps

K2CO3 (232 mg, 1.682 mmol) and bis(triphenylphosphine) palladium(II) dichloride (39.3 mg, 0.056 mmol) were each rapidly added in sequence to a suspension of 7-chloro-5-methyl-2-[2-(1-methyl-1H-benzoimidazol-2-yl)-ethyl]-3,5-dihydro-2H-pyrrolo[3,4-c]pyridine-1,6-dione (200 mg, 0.561 mmol, see Example c8)) and pyridin-3-ylboronic acid (103 mg, 0.841 mmol) in DMF (3 ml)/water (0.600 ml). The reaction was heated in a microwave at about 120° C. for about 20 min. The reaction was cooled to r.t., DCM (15 ml) and DMF (1 ml) were added, the resulting mixture was filtered and the filtrate was concentrated by evaporating DCM. The concentrate was cooled to r.t., the crystallized solid was filtered off, washed with water and dried to afford the title compound (50 mg, 0.125 mmol, 22.33% yield).

Provenance & Evidence