N-methyl-2-pyrrolidone → Methyl 5-[3-fluoro-4-(trifluoromethoxy)phenyl]-1-(thiomorpholin-4-ylcarbonyl)piperidine-3-carboxylate

Participants

Reaction Conditions

Reaction Steps

2.40 g (4.93 mmol) of the compound from Example 93A, 3.56 g (34.5 mmol) of thiomorpholine and 3.0 ml (2.32 g, 17.3 mmol) of N,N-diisopropylethylamine were added to 28 ml of 1-methyl-2-pyrrolidone and heated in 2 portions in a single-mode microwave (Emrys Optimizer) at 150° C. for 1 h. For workup, the reaction solutions were combined and admixed with water. After addition of ethyl acetate and phase separation, the organic phase was washed with saturated aqueous sodium chloride solution, dried (magnesium sulphate), filtered and concentrated under reduced pressure. Yield: 1.97 g (89% of theory)

Provenance & Evidence