Dimethylbarbituric acid → 2-Methoxy-6-(pyrrolidin-3-YL)pyridine

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-methoxy-6-[1-(prop-2-en-1-yl)pyrrolidin-3-yl]pyridine a1-55 (218 mg, 1 mmol, 1 eq) in dichloromethane (3 ml) are added 1,3-dimethylbarbituric acid (470 mg, 3 mmol, 3 eq) and Pd(PPh3)4 (20 mg) and the mixture is warmed overnight at 40° C. The reaction mixture is loaded on an ion exchange acidic resin cartridge, washed with methanol (2×50 ml) and then released with a 1M solution of ammonia in methanol (20 ml) to afford 150 mg of crude 2-methoxy-6-(pyrrolidin-3-yl)pyridine a1-59 that is used in the next step without any further purification.

Provenance & Evidence