反应详情

In a similar manner to Step 2 of Example 6, 4-(3-thiophenesulfonyloxy)-5-methoxy-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinone (0.219 g, 0.385 mmol) was dissolved in acetonitrile (6.0 mL), and the solution was treated with dimethylamine hydrochloride (0.630 g, 7.70 mmol), triethylamine (1.10 mL, 7.70 mmol), acetic acid (0.441 mL, 7.70 mmol) and sodium triacetoxyborohydride (0.245 g, 1.16 mmol), followed by purification of the residue by flash column chromatography (chloroform/methanol=85/15) to obtain 4-(3-thiophenesulfonyloxy)-5-methoxy-7-[1-(tert-butoxycarbonyl)-5-(dimethylaminomethyl)indol-2-yl]isoindolinone (0.104 g, 45%).

1. customfollowed by purification of the residue by flash column chromatography (chloroform/methanol=85/15)