Triethylamine → 2-cyclopropyl-7-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-6-(2-fluorophenyl)-5-methyl-1,3-benzoxazole-4-carbonitrile

Participants

Reaction Conditions

Reaction Steps

2-Cyclopropyl-7-fluoro-6-(2-fluorophenyl)-5-methyl-1,3-benzoxazole-4-carbonitrile (I-175) (147 mg, 0.47 mmol) was dissolved in dimethyl sulfoxide (3 ml), then at room temperature, triethylamine (99 μl, 0.71 mmol) and (3S)-3-(dimethylamino)pyrrolidine (78 μl, 0.62 mmol) were added. The solution was stirred under nitrogen atmosphere at 90° C. for 10 hours. After cooling to room temperature, the reaction liquid was fractionated with ethyl acetate and an aqueous saturated sodium hydrogencarbonate solution.

Provenance & Evidence