Morpholine → 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

Palladium diacetate (65.5 mg, 0.292 mmol), Xantphos (169 mg, 0.292 mmol) and Cs2CO3 (285 mg, 0.875 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 morpholine (76 mg, 0.875 mmol) in dioxane (1 ml). The reaction was heated in a microwave at about 120° C. for about 40 min. The solvent was removed and the resulting mixture was purified by preparative HPLC (system: Waters 2767 PHW003, eluent: MeCN/ammonium acetate buffer (gradient: 10:90 to 35:65 over 15 min), column: Boston Analytics, C-18, 10 μm, 21×250 mm) to afford the title compound (24.1 mg, 0.061 mmol, 21.00% yield).

Provenance & Evidence