Boron tribromide → HCID 178428097, compound

Participants

Reaction Steps

(S)-2-(1-((6-Amino-5-(2-methoxy-6-(trifluoromethyl)pyridin-4-yl)pyrimidin-4-yl)amino)ethyl)-5-methyl-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4(3H)-one (40 mg, 0.07 mmol) was dissolved in dichloromethane (1 ml). A solution of boron tribromide (1M in dichloromethane, 223 μl, 0.22 mmol) was added dropwise and the reaction mixture was stirred at room temperature overnight. Further boron tribromide (1M in dichloromethane, 223 μl, 0.22 mmol) was added and the reaction mixture stirred at room temperature an extra night. The reaction mixture was then diluted with dichloromethane and washed with a solution of 4% sodium bicarbonate, water, brine and dried over sodium sulphate, filtered and evaporated under reduced pressure. The product was purified by reverse phase using SP1® Purification System to give 8 mg (20% yield) of the title compound as a white solid. Purity 99%.

Provenance & Evidence