تفاعل #2254233

معادلة التفاعل

triethylamine

methanesulfonyl chloride

(5-fluoro-1H-indol-7-ylmethyl)-(2-hydroxyethyl)-carbamic acid tert-butyl ester

→

desired compound

المردود 100.8%

Methanesulfonic acid 2-[tert-butoxycarbonyl-(5-fluoro-1H-indol-7-ylmethyl)-amino]-ethyl ester

المردود 100.8%

المذيبات

ethyl acetate

dichloromethane

ظروف التفاعل

المعالجة

1. 1
   غسيلwash with sequentially with saturated aqueous sodium bicarbonate (200 mL×3) and saturated aqueous sodium chloride (200 mL×2)
2. 2
   تجفيفDry the organic phase over sodium sulfate
3. 3
   تركيزconcentrate under reduced pressure

الإجراء التجريبي

Add triethylamine (4.64 mL, 33.3 mmol) followed by methanesulfonyl chloride (1.29 mL, 16.65 mmol) to a solution of (5-fluoro-1H-indol-7-ylmethyl)-(2-hydroxyethyl)-carbamic acid tert-butyl ester (4.9 g, assume 15.14 mmol) in dichloromethane (70 mL) at 0° C. Stir the reaction mixture for 30 minutes at 0° C. Dilute with ethyl acetate (200 mL), wash with sequentially with saturated aqueous sodium bicarbonate (200 mL×3) and saturated aqueous sodium chloride (200 mL×2). Dry the organic phase over sodium sulfate and concentrate under reduced pressure to provide the desired compound as a yellow brown oil (5.9 g, >100%).

المصدر