反应详情

In a similar manner to Step 2 of Example 6, 4-methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-4-formylindol-2-yl]isoindolinone (0.262 g, 1.17 mmol) was dissolved in acetonitrile (15.0 mL), and the solution was treated with 2.0 mol/L methylamine-THF solution (5.20 mL, 10.5 mmol), acetic acid (0.600 mL, 10.5 mmol) and sodium triacetoxyborohydride (0.555 g, 2.62 mmol), followed by purification of the residue by flash column chromatography (chloroform/methanol=3/1) to obtain 4-methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-4-(dimethylaminomethyl)indol-2-yl]isoindolinone (0.0839 g, 30%).

1. customfollowed by purification of the residue by flash column chromatography (chloroform/methanol=3/1)