Boron tribromide → HCID 90102388, compound

Participants

Reaction Steps

(S)-2-(1-((6-Amino-5-(1-((4-methoxyphenyl)sulfonyl)-1H-indol-6-yl)pyrimidin-4-yl)amino)ethyl)-5-methyl-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4(3H)-one (100 mg, 0.14 mmol) was dissolved in dichloromethane (1 ml). A solution of boron tribromide (1M in dichloromethane, 952 μL, 0.95 mmol) was added dropwise and the reaction was stirred at room temperature overnight. A solution of boron tribromide (1M in dichloromethane, 1.4 ml, 1.4 mmol) was added dropwise and the reaction was heated at 60° C. overnight. The mixture was diluted with ethyl acetate and washed with a 4% solution of sodium bicarbonate, water, brine and dried over sodium sulphate, filtered and evaporated under reduced pressure. The product was purified by reverse phase chromatography using SP1® Purification System to give 53 mg (61% yield) of the title compound. Purity 99%. LRMS (m/z): 633 (M+1)+.

Provenance & Evidence