反应详情

Dissolve (±)-2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-4-(6-fluoro-pyridin-2-ylmethyl)-1,2,3,4-tetrahydro-cyclopenta[b]indole-7-carbonitrile (5.31 g, 12.2 mmol) in ethanol (15 mL)/tetrahydrofuran (85 mL). Add hydrazine monohydrate (4.43 ml, 91.2 mmol, 7.50 equivalents) and stir at room temperature under nitrogen overnight. Dilute with ethyl acetate (150 ml), filter off white solids, wash the organic layer with 10% potassium carbonate twice, dry over anhydrous sodium sulfate, filter, and concentrate to obtain the title compound as an orange oil (3.42 g, 91%). LCMS 307.0 (M+1), 305.0 (M−1).

1. filtrationfilter off white solids
2. washwash the organic layer with 10% potassium carbonate twice
3. dry with materialdry over anhydrous sodium sulfate
4. filtrationfilter
5. concentrationconcentrate