Diisopropylethylamine → 6-Methyl-4-oxo-5-(3-trifluoromethyl-phenyl)-1,4-dihydro-pyridine-3-carboxylic acid (5-methanesulfonyl-pyridin-2-ylmethyl)-amide

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Reaction Steps

A solution of 6-methyl-4-oxo-5-(3-trifluoromethyl-phenyl)-1,4-dihydro-pyridine-3-carboxylic acid (preparation 5b, 0.800 g, 2.69 mmol), HBTU (1.07 g, 2.81 mmol), DIPEA (1.37 mL, 8.08 mmol) in NMP (5 mL) is stirred for 30 min. Then, C-(5-methanesulfonyl-pyridin-2-yl)-methylamine (0.55 g, 2.95 mmol) is added and the reaction mixture is stirred for 18 h at room temperature. The reaction mixture is diluted with a small amount of MeOH. Upon addition of water a precipitate forms which is collected by filtration and dried. Yield: 0.78 g (62% of theory); ESI mass spectrum: [M+H]+=466; Retention time HPLC: 1.09 min (V003—003).

Provenance & Evidence