Formaldehyde → HCID 53853843, compound

Participants

Reaction Steps

Formaldehyde (132 mg, 1.65 mmol, 37% in water) was added to a solution of of crude 2-[1-(1-tert-butoxycarbonyl-piperidin4-yl)-ethyl]-malonic acid monoethyl ester (416 mg) in methylene chloride (2 mL) at 0° C. Diethylamine (153 μL, 1.47 mmol) was added dropwise and the mixture was stirred at room temperature over night. EtOAc was added and the mixture was washed with water and saturated NaHCO3, dried and concentrated under reduced pressure. The crude was purified by flash chromatography (toluene/EtOAc, 3:1) to give 4-(2-ethoxycarbonyl-1-methyl-allyl)-piperidine-1-carboxylic acid tert-butyl ester (0.18 g, 49% over two steps).

Provenance & Evidence