Potassium tert-butoxide → 5-[3-Fluoro-4-(2,2,2-trifluoroethyl)phenyl]-1-(thiomorpholin-4-ylcarbonyl)piperidine-3-carboxylic acid

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Reaction Conditions

Reaction Steps

To a solution of 4.29 g (9.57 mmol) of the compound from Example 78A in methanol (190 ml) were added, at RT, 10.7 g (112 mmol) of potassium tert-butoxide. The mixture was stirred at 60° C. overnight. For workup, the methanol was removed under reduced pressure, and the residue was admixed with water and acidified (pH=1) with aqueous 1 N hydrochloric acid solution. The mixture was extracted with ethyl acetate, and the organic phase was dried with magnesium sulphate, filtered and concentrated under reduced pressure. Yield: 3.94 g (76% of theory, purity 80%).

Provenance & Evidence