Dimethylformamide → HCID 22313088, compound

Participants

Reaction Steps

To a solution of compound B (820 mg, 3 mmol) in dimethyl formamide (10 mL) were added EDCI (700 mg, 3.6 mmol), HOBt (460 mg, 3 mmol), methoxylamine hydrochloride (370 mg, 3.6 mmol) and triethylamine (0.9 mL). After stirring for 1 h at RT, the mixture was diluted with ethyl acetate and washed with water, dried and concentrated. The solid obtained was dissolved in dichloromethane (2.5 mL) and TFA (2.5 mL) was added. After 2 h, the mixture was concentrated, the residue was dissolved in ethyl acetate and washed with saturated NaHCO3 to afford 5-amino-2-methyl-4-fluoro-N-methoxybenzamide (520 mg). LC/MS; (M+H)+=199.2.

Provenance & Evidence