Methanol → Tert-butyl-[(2r,3r)-8-(methylsulfonyl)-3-(2,4,5-trifluorophenyl)-1,2,3,4-tetrahydropyrido-[1,2-a]benzimidazol-2-yl]carbamate

Participants

Reaction Steps

To a solution containing 41 mg (0.088 mmol) of the product from Step B in 6.0 mL of methanol was added 160 mg (0.26 mmol) of oxone as a 2 mL aqueous solution. The reaction mixture was stirred at ambient temperature for 16 h, then diluted with 50 mL of ethyl acetate and washed sequentially with 0.5N aqueous sodium bicarbonate solution and saturated aqueous brine (50 mL each), dried over sodium sulfate, filtered and the solvent evaporated in vacuo to yield a crude solid. Purification by reverse phase HPLC (YMC Pro-C18 column, gradient elution, 5% to 80% acetonitrile/water with 0.1% TFA) afforded the pure title compound as a white foam. LC/MS 496.1 (M+1).

Provenance & Evidence