تفاعل #49290

معادلة التفاعل

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

sodium carbonate

1-(2-hydroxyethyl)piperazine

acetic acid

sodium triacetoxyborohydride

→

4-chloro-7-(1-(tert-butoxycarbonyl)-5-[4-(2-hydroxyethyl)piperazin-1-ylmethyl]indol-2-yl)isoindolinone

المردود 111.9%

المذيبات

acetonitrile

water

ظروف التفاعل

المعالجة

1. 1
   استخلاصby extracting with ethyl acetate
2. 2
   غسيلThe organic layer was washed with saturated brine
3. 3
   تجفيفdried over anhydrous sodium sulfate
4. 4
   أخرىThe solvent was evaporated under reduced pressure

الإجراء التجريبي

In a similar manner to Step 2 of Example 6, 4-chloro-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinone (20.7 mg, 0.0504 mmol) was dissolved in acetonitrile (1 mL), and the solution was treated with 1-(2-hydroxyethyl)piperazine (28 mg, 0.22 mmol), acetic acid (0.232 mL, 4.05 mmol) and sodium triacetoxyborohydride (116 mg, 0.547 mmol). The reaction mixture was added with water and sodium carbonate, followed by extracting with ethyl acetate. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure to obtain 4-chloro-7-(1-(tert-butoxycarbonyl)-5-[4-(2-hydroxyethyl)piperazin-1-ylmethyl]indol-2-yl)isoindolinone (29.6 mg).

المصدر