Formaldehyde → HCID 20773488, compound

Participants

Reaction Steps

To a solution of (R)-1-(5-aminohexyl)-8-(N-BOC-aminomethyl)-3-methylxanthine (0.4 g, 1.0 mmol) in methanol (10 ml) was added formaldehyde (37% in water) (0.4 ml) followed by sodium cyanoborohydride (0.1 g, 1.5 mmol). After stirring at room temperature for 1 hour, the solvent was evaporated under reduced pressure. The crude product was purified by flash chromatography on silica gel eluting with ammonium hydroxide (37% in water)-methanol-ethyl acetate mixture (1:5:10) to give (R)-1-(5-dimethylaminohexyl)-8-(N-BOC-aminomethyl)-3-methylxanthine (0.20 g, 47% yield) as an oil.

Provenance & Evidence