6-chloro-2-[4-(2-chlorophenyl)-2-{[5-(trifluoromethyl)-2H-tetrazol-2-yl]methyl}pyrimidin-5-yl]-8-methyl-4H-3,1-benzoxazin-4-one → N-[4-chloro-2-methyl-6-(methylcarbamoyl)phenyl]-4-(2-chlorophenyl)-2-{[5-(trifluoromethyl)-2H-tetrazol-2-yl]methyl}pyrimidine-5-carboxamide

Participants

Reaction Conditions

Reaction Steps

100 mg (0.18 mmol) of 6-chloro-2-[4-(2-chlorophenyl)-2-{[5-(trifluoromethyl)-2H-tetrazol-2-yl]methyl}pyrimidin-5-yl]-8-methyl-4H-3,1-benzoxazin-4-one were initially charged in 3 ml of THF, and 0.234 ml (0.46 mmol) of a 2 molar methylamine/THF solution was added at RT. The reaction mixture was then stirred at 45° C. for 15 min. After cooling, the mixture was concentrated and purified chromatographically on silice gel using cyclohexane/ethyl acetate. 48 mg (40% of theory; content 89%) of the desired product were isolated.

Provenance & Evidence