Pyridine → HCID 17989375, compound

Participants

Reaction Conditions

Reaction Steps

4-Bromophthalic anhydride [Apin] (2.27 g, 10 mmol) was dissolved in 1,2-dichloromethane (8 ml), and pyridine (10 mmol, 0.81 ml) was added, followed by 4-(2-diisopropylamino-ethoxy)-3-methoxy-phenylamine [Patent WO-9901127] (2.44 g, 10 mmol) and a catalytic amount of 4-dimethylaminopyridine [Aldrich]. The mixture was heated for 16 h at 85° C. The mixture was evaporated in vacuo and applied to a Biotage Flash40M cartridge, (eluting with dichloromethane-methanol-aqueous ammonia) to give the 5-bromo-2-[4-(2-diisopropylamino-ethoxy)-3-methoxy-phenyl]-isoindole-1,3-dione 3.05 g, 68%, as the trifluoroacetate salt;

Provenance & Evidence