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反应机理
反应操作
A 10 mL threaded Pyrex test tube equipped with a magnetic stirring bar, a rubber septum, and argon inlet needle was charged with Boc2O (223 mg, 1.02 mmol). A solution of mono-methyl succinate (9a) (54.0 mg,0.409 mmol), indole (1) (120 mg, 1.02 mmol), DMAP (2.5 mg, 0.02 mmol), and 2,6-lutidine (4.7μL, 0.04 mmol) in MeCN (0.9 mL) were added to the test tube at room temperature. Then, the reaction mixture was warmed to 28°C by water bath. After stirring at 28°C for 24 h, the resulting mixture was concentrated under reduced pressure to give a crude oil, which was purified by silica gel column chromatography (hexanes/AcOEt = 5:1) to give N-acylindole 10a (87.1 mg, 0.377mmol, 92%)