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

Participants

Reaction Conditions

Reaction Steps

Bis(triphenylphosphine)palladium(II) dichloride (14.88 mg, 0.021 mmol) and K2CO3 (176 mg, 1.27 mmol) were added to a suspension of 7-chloro-5-methyl-2-(2-quinolin-2-yl-ethyl)-3,5-dihydro-2H-pyrrolo[3,4-c]pyridine-1,6-dione (150 mg, 0.424 mmol, see Example c4)) and pyridine-3-ylboronic acid (104 mg, 0.848 mmol) in DMF (3 ml)/water (0.6 ml) and the mixture was heated in a microwave at 130° C. for 30 min. The solvent was removed and the resulting solid was purified by preparative HPLC (system: Gilson 281(PHG008), eluent: MeCN/aqueous 0.1% TFA solution (gradient: 30:70 to 80:20 over 15 min), column: Boston symmetrix ODS-R, C-18, 10 nm, 21.2×250 mm) to afford the title compound (150 mg, 89% yield).

Provenance & Evidence