反应详情

温度

30 °C

To the stirred solution of benzyne precursor 1 (100 mg, 0.33 mmol) and malonamide ester 2 (40 mg, 0.16 mmol) in anhydrous MeCN (2 mL) was added NaHCO3 (28 mg, 0.33 mmol), CsF (200 mg, 1.34 mmol). Reaction mixture was allowed to stir at room temperature 30° C. for 48 hrs. The reaction mixture was concentrated in vacuo and directly loaded on silica gel and purified by using gradient solvent combination of ethyl acetate/Pet ether to yield a low melting solid compound 4 (43 mg, 65%).

1. customReaction mixture
2. concentrationThe reaction mixture was concentrated in vacuo
3. custompurified