Ammonia → (S)-tert-Butyl (3-(benzyloxy)-1-(4-oxo-3-phenyl-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)propyl)carbamate

Participants

Reaction Steps

(S)-tert-Butyl (4-(benzyloxy)-1-oxo-1-((2-(phenylcarbamoyl)-1H-pyrrol-1-yl)amino)butan-2-yl)carbamate (1.57 g, 3.19 mmol) was treated with triphenylphosphine (1.17 g, 4.46 mmol), bromine (229 μl, 4.47 mmol), triethylamine (1.78 mL, 12.77 mmol) and a solution of ammonia solution (7M in methanol, 150 mL, 1000 mmol) according to the method of Preparation 5b. The residue was purified using SP1® Purification System (0% to 30%, hexane-ethyl acetate) to give 0.81 g (53.5%) of the title compound as a white solid. Purity 100%.

Provenance & Evidence