反应详情

Diethyl azodicarboxylate (650 μL, 4.13 mmol, 2.0 eq) is added at 0° C. to a stirred solution of {trans-4-[2-hydroxy-3-(3-hydroxy-6-methoxy-[1,5]naphthyridin-4-yl)-propyl]-cyclohexyl}-carbamic acid tert-butyl ester (890 mg, 2.06 mmol, 1.0 eq) in tetrahydrofuran (100 mL), followed by triphenylphosphine (1.08 g, 4.13 mmol, 2.0 eq). After 1 hour stirring at room temperature, solvent is removed and the crude is purified by column chromatography (silica gel, eluent: petroleum ether:ethyl acetate, 5:1, v/v) to afford [trans-4-(8-methoxy-1,2-dihydro-3-oxa-5,9-diaza-cyclopenta[a]naphthalen-2-ylmethyl)-cyclohexyl]-carbamic acid tert-butyl ester as a white solid (420 mg, 49% yield).

1. customsolvent is removed
2. customthe crude is purified by column chromatography (silica gel, eluent