反应详情

A mixture of 5-(1-benzylpiperidin-3-yloxy)-3-(1-naphthylsulfonyl)-1H-indazole (0.7 g, 1.4 mmoles), 10% Pd/C and concentrated HCl (1 mL) in THF and methanol was hydrogenated in a Parr hydrogenation bottle at 52 lb/in2 for 72 hours. TLC showed about 30% conversion into desired product. The reaction mixture was filtered through Celite, and the filtrate was concentrated. The concentrate, a mixture of starting material and product, was then separated by reverse phase chromatography on C18 column, using as eluent 10-100% H2O/AcCN, to afford the title compound as an off-white solid, 0.16 g, mp 178-180° C., identified by HNMR and mass spectral analyses, MS (ES) m/z 406.1.