Triethylamine → HCID 58811479, compound

Participants

Reaction Conditions

Reaction Steps

Mix 4-bromo-N1-(1,1-dimethyl-2-morpholin-4-yl-ethyl)-benzene-1,2-diamine (3.76 g, 11.5 mmol), triethylamine (4.6 mL, 34.4 mmol) in THF (150 mL). Cool to 0° C. and carefully add solid triphosgene (2.0 g, 6.9 mmol). Allow the reaction to warm to room temperature and stir for 18 h. Cautiously quench the reaction with aqueous K2CO3 and extract into EtOAc. Dry (MgSO4) and concentrate to give 3.4 g yellow solid. Purify by column chromatography using 3% 3N NH3 in MeOH/methylene chloride to give 2.25 g (55%) title compound as a white solid, MS (es) 354, 356 (M+1), 352, 354 (M−1). HPLC(ISO80-10M) t=1.55.

Provenance & Evidence