Acetic Acid → HCID 117701770, compound

Participants

Reaction Conditions

Reaction Steps

A mixture composed of 7-hydroxy-3,8-dimethyl-2-[(2R)-pyrrolidin-2-yl]-4H-chromen-4-one hydrochloride (78 mg, 0.30 mmol) obtained in Example 2-3, 90% paraformaldehyde (50 mg, 1.50 mmol), magnesium sulfate (60 mg), and acetic acid (17 μL, 0.30 mmol) was stirred at 50° C. for 5 minutes. Then, sodium cyanoborohydride (43 mg, 0.66 mmol) was added thereto, and the mixture was stirred at 50° C. for 3 hours. Insoluble matter in the reaction solution was filtered off and then washed with methanol. The filtrate was concentrated under reduced pressure, and the obtained residue was purified by reverse-phase HPLC to obtain 23 mg of the title compound (yield: 27%).

Provenance & Evidence