tert-butyl 3-(4-nitro-1H-pyrazol-1-yl)azetidine-1-carboxylate → 4-Amino-1-(1-Boc-azetidin-3-yl)-1H-pyrazole

Participants

Reaction Steps

To a solution of tert-butyl 3-(4-nitro-1H-pyrazol-1-yl)azetidine-1-carboxylate (5.3 g) obtained in Step B of Example 131 in ethanol (30 mL) was added 5% palladium-carbon (4.2 g), and the mixture was stirred at room temperature for 2 hr under hydrogen atmosphere (at normal pressures). The palladium-carbon was removed by filtration through Celite, the solvent was evaporated under reduced pressure, and the residue was purified by silica gel column chromatography (NH, hexane/ethyl acetate) to give the title compound (2.1 g).

Provenance & Evidence