تفاعل #49585

معادلة التفاعل

4-methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-4-formylindol-2-yl]isoindolinone

2-methoxyethylamine

acetic acid

sodium triacetoxyborohydride

→

4-methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-4-(2-methoxyethylaminomethyl)indol-2-yl]isoindolinone

المردود 34.4%

المذيبات

acetonitrile

ظروف التفاعل

المعالجة

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

الإجراء التجريبي

In a similar manner to Step 2 of Example 6, 4-methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-4-formylindol-2-yl]isoindolinone (0.252 g, 0.503 mmol) was dissolved in acetonitrile (15.0 mL), and the solution was treated with 2-methoxyethylamine (0.875 mL, 10.1 mmol), acetic acid (0.576 mL, 10.1 mmol) and sodium triacetoxyborohydride (0.533 g, 2.52 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-(2-methoxyethylaminomethyl)indol-2-yl]isoindolinone (0.0968 g, yield 34%).

المصدر