4-[1-(4-Methoxybenzyl)amino-5-isoquinolyl]amino-1-(tert-butoxycarbonyl)piperidine → 4-(1-Amino-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidine

Participants

Reaction Steps

A solution of Intermediate 132 (270 mg) in 95% trifluoroacetic acid (5 ml) was stirred at 50° C. for 16 hours, and the solvent was evaporated under reduced pressure. The residue was added with dioxane (3 ml), 2 N aqueous sodium hydroxide (1 ml) and 2 di-t-butyl dicarbonate (393 mg) and stirred at room temperature for 1 hour. The solvent was evaporated under reduced pressure, and then the residue was purified by silica gel column chromatography (n-hexane:ethyl acetate:isopropylamine=5:5:1) to obtain the title compound (199 mg).

Provenance & Evidence