反応 #449697

反応方程式

Ethyl acetate

7-[[4-[(1-t-Butoxycarbonyl-4-piperidyl)oxy]anilino]methyl]-2-naphthalenecarbonitrile

ethanesulfonyl chloride

→

N-[4-[(1-t-butoxycarbonyl-4-piperidyl)oxy]phenyl]-N-[(7-cyano-2-naphthyl)methyl]ethanesulfonamide

溶媒

pyridine

反応条件

後処理

1. 1
   workup.WAITat room temperature for 3 hours
2. 2
   洗浄The mixture was washed with 10% citric acid aqueous solution and brine in that order
3. 3
   乾燥dried over anhydrous sodium sulfate
4. 4
   その他evaporated
5. 5
   その他The resulting residue was purified by silica gel column chromatography

実験手順

7-[[4-[(1-t-Butoxycarbonyl-4-piperidyl)oxy]anilino]methyl]-2-naphthalenecarbonitrile obtained in Reference Example 2 (150 mg) was dissolved in 1 ml of pyridine, 211 mg of ethanesulfonyl chloride was added to the solution, and the mixture was stirred at 0° C. for 20 minutes and then at room temperature for 3 hours. Ethyl acetate was added to the reaction solution. The mixture was washed with 10% citric acid aqueous solution and brine in that order, dried over anhydrous sodium sulfate, and then evaporated. The resulting residue was purified by silica gel column chromatography using hexane:ethyl acetate (75:25) as the eluent to give 176 mg of N-[4-[(1-t-butoxycarbonyl-4-piperidyl)oxy]phenyl]-N-[(7-cyano-2-naphthyl)methyl]ethanesulfonamide.

出典