反应详情

After stirring a solution of trans-8-chloro-1-[4-(3-fluoro-pyridin-2-yl)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene (50.0 mg, 0.126 mmol), acetone (0.019 ml, 0.251 mmol) and acetic acid (0.014 ml, 0.25 mmol) in 1,2-dichloroethane (1.3 ml) at room temperature for 5 h, sodium triacetoxyborohydride (58.6 mg, 0.276 mmol) was added. Stirring for further 20 h was followed by quenching with methanol (1 ml) and N-ethyldiisopropylamine (0.044 ml, 0.25 mmol). The reaction mixture was stirred for 30 minutes and concentrated in vacuo. Preparative RP-HPLC with water (0.05% formic acid)/methanol as eluent gave the title compound (40 mg, 72%) as white solid. MS m/e: 440 ([M+H]+)

1. stirringThe reaction mixture was stirred for 30 minutes
2. concentrationconcentrated in vacuo