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 (0.0650 g, 0.114 mmol) was dissolved in acetonitrile (5.0 mL), and the solution was treated with pyrrolidine (0.191 mL, 2.29 mmol), acetic acid (0.131 mL, 2.29 mmol) and sodium triacetoxyborohydride (0.0730 g, 0.343 mmol), followed by purification of the residue by flash column chromatography (chloroform/methanol=85/15, 80/20) to obtain 4-(3-thiophenesulfonyloxy)-5-methoxy-7-[1-(tert-butoxycarbonyl)-5-(pyrrolidin-1-ylmethyl)indol-2-yl]isoindolinone (0.0501 g, 70%).

1. customfollowed by purification of the residue by flash column chromatography (chloroform/methanol=85/15, 80/20)