Triethylamine → 3-Methyl 1-(4-nitrophenyl) 5-[3-fluoro-4-(2,2,2-trifluoroethyl)phenyl]piperidine-1,3-dicarboxylate

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Reaction Steps

A solution of 4.00 g (9.52 mmol, purity 76%) of the compound from Example 76A in dichloromethane (111 ml) was admixed with 4.65 ml (3.37 g, 33.3 mmol) of triethylamine and then, at 0° C., admixed with 1.92 g (9.52 mmol) of 4-nitrophenyl chloroformate. The mixture was warmed to RT and stirred for 2 h. The reaction solution was washed with saturated aqueous sodium hydrogencarbonate solution and water, and the organic phase was dried over magnesium sulphate, filtered and concentrated under reduced pressure. Yield: 5.42 g (94% of theory, purity 80%)

Provenance & Evidence