4-Amino-1-Boc-piperidine → HCID 66693371, compound

Participants

Reaction Steps

Tris(dibenzylideneacetone)dipalladium (30 mg; 0.03 mmol), 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (62 mg; 0.10 mmol), sodium tert-butoxide (240 mg; 2.50 mmol), 5-(4-bromo-phenyl)-1-methyl-1H-tetrazole (406 mg; 1.70 mmol, prepared in accordance with Example 18) and 4-amino-piperidine-1-carboxylic acid tert-butyl ester (421 mg; 2.1 mmol) are suspended in dry toluene (7 mL) and the mixture is irradiated in a mono-mode microwave oven for 20 min. at 120° C. The mixture is then cooled down to room temperature, is diluted with ethyl acetate (15 mL), is filtered and is concentrated under reduced pressure. The crude residue is finally purified by chromatography on silica gel (dichloromethane:methanol 100:0 to 98:2) to afford the desired product (401 mg; 1.12 mmol).

Provenance & Evidence