反応 #11718

反応方程式

2-chloro-1-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-ethanone

4-(5-chloro-2-hydroxy-phenyl)-4-oxo-butyric acid ethyl ester

1,5,7-triazabicyclo[4,4,0]dec-5-ene bound to polystyrene

→

title compound

収率 45.0%

4-(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-4-oxo-butyric acid ethyl ester

収率 45.0%

溶媒

acetonitrile

反応条件

後処理

1. 1
   ろ過The reaction mixture was filtered through a glass frit
2. 2
   濃縮concentrated in vacuo
3. 3
   その他purified via flash chromatography on silica gel

実験手順

A solution of 2-chloro-1-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-ethanone (0.11 g, 0.36 mmol), 4-(5-chloro-2-hydroxy-phenyl)-4-oxo-butyric acid ethyl ester (0.11 g, 0.43 mmol) and 1,5,7-triazabicyclo[4,4,0]dec-5-ene bound to polystyrene crosslinked with 2% DVB (0.21 g, 0.54 mmol) in acetonitrile (1.8 mL) was stirred at ambient temperature for 12 hours. The reaction mixture was filtered through a glass frit, concentrated in vacuo and purified via flash chromatography on silica gel to give the title compound (0.084 g).

出典