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

Participants

Reaction Conditions

Reaction Steps

K2CO3 (121 mg, 0.875 mmol) and bis(triphenylphosphine) palladium(II) dichloride (20.48 mg, 0.029 mmol) were each rapidly added in sequence to a suspension of 7-chloro-2-(2-imidazo[1,2-a]pyridin-2-yl-ethyl)-5-methyl-3,5-dihydro-2H-pyrrolo[3,4-c]pyridine-1,6-dione (100 mg, 0.292 mmol, see Example c5)) and pyridin-3-ylboronic acid (53.8 mg, 0.438 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 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 and dried to afford the title compound (40 mg, 0.104 mmol, 35.6% yield).

Provenance & Evidence