Formaldehyde → HCID 11855214, compound

Participants

Reaction Conditions

Reaction Steps

3 ml of acetic acid, 24 μl of a formaldehyde aqueous solution (36%) and 47 μl of N-butyl-N-methylamine were added to 150 mg of ethyl 1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)thiazol-2-yl]carbamoyl}-2-pyridyl)piperidine-4-carboxylate, and the mixture was stirred at 90° C. for 18 hours. After the solvent was distilled off under reduced pressure, a saturated sodium hydrogencarbonate aqueous solution was added. The mixture was extracted with chloroform, and dried over magnesium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was purified by silica gel column chromatography using hexane:EtOAc (7:1 to 5:1) as an elution solvent to obtain 147 mg of ethyl 1-(5-{[5-{[butyl(methyl)amino]methyl}-4-(4-chlorothiophen-2-yl)thiazol-2-yl]carbamoyl}-3-chloro-2-pyridyl)piperidine-4-carboxylate.

Provenance & Evidence