Methyl N-(triethylammoniosulfonyl)carbamate → 1-(Morpholin-4-ylcarbonyl)-5-[4-(trifluoromethyl)phenyl]piperidine-3-carbonitrile

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Reaction Conditions

Reaction Steps

Under argon, 3.83 g (16.1 mmol) of Burgess reagent were added to a solution of 4.42 g (11.5 mmol) of the compound from Example 82A in 208 ml of tetrahydrofuran. The mixture was stirred at 70° C. for 1 h. For work-up, the solvent was removed under reduced pressure and the residue was taken up in ethyl acetate. The organic phase was washed successively with water and saturated aqueous sodium chloride solution, dried over magnesium sulphate and concentrated. Yield: 4.19 g (99% of theory)

Provenance & Evidence