反応 #49463

反応方程式

4-Hydroxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone

triethylamine

trifluoromethanesulfonyl chloride

→

4-trifluoromethanesulfonyloxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone

収率 93.0%

溶媒

dichloromethane

反応条件

後処理

1. 1
   温度cooling
2. 2
   ろ過The reaction mixture was filtered
3. 3
   workup.ADDITIONthe filtrate was added with water
4. 4
   抽出extracted with ethyl acetate
5. 5
   洗浄The organic layer was washed with saturated brine
6. 6
   乾燥dried over anhydrous sodium sulfate
7. 7
   その他The solvent was evaporated under reduced pressure

実験手順

4-Hydroxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (80.0 mg, 0.173 mmol) was suspended in dichloromethane (4.8 mL), and the suspension was added with triethylamine (0.072 mL, 0.52 mmol) and trifluoromethanesulfonyl chloride (0.022 mL, 0.21 mmol) under ice-cooling, followed by stirring for 0.8 hour. The reaction mixture was filtered and the filtrate was added with water and extracted 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-trifluoromethanesulfonyloxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (95.4 mg, yield 93%).

出典