Formamide → HCID 136336816, compound

Participants

Reaction Steps

1.00 g of methyl 3-amino-6-[2-methyl-3-(2-trimethylsilanylethoxymethyl)-3H-imidazo[4,5-b]pyridin-6-yl]pyridine-2-carboxylate in 16 ml of formamide are heated at 130° C. under nitrogen in a flask until the reaction is complete (HPLC check, about 48 hours). The excess formamide is distilled off (120° C., 1 mbar). The residue is dissolved in dichloromethane, washed with water, dried and purified by means of column chromatography (gradient EA: methanol 0-50% in 15 min), giving 0.40 g of 6-[2-methyl-3-(2-trimethylsilanylethoxymethyl)-3H-imidazo[4,5-b]pyridin-6-yl]-3H-pyrido[3,2-d]pyrimidin-4-one as reddish solid (yield 36%, content 95%); MS-FAB (M+H+)=409.1; Rf (polar method): 2.01 min.

Provenance & Evidence