反応 #418023

反応方程式

2-fluoro-ethanol

2-[4-(2-chloro-pyrimidin-5-ylethynyl)-phenyl]-N-ethyl-propionamide

sodium hydride

→

desired product

N-Ethyl-2-{4-[2-(2-fluoro-ethoxy)-pyrimidin-5-ylethynyl]-phenyl}-propionamide

溶媒

1,4-dioxane

1,4-dioxane

反応条件

後処理

1. 1
   その他After that time, the solvent is evaporated
2. 2
   その他the residue s purified by HPLC (preparative column: Sunfire, eluent A: water+0.1% TFA, eluent B: MeOH)

実験手順

To 13 mg (0.21 mmol) 2-fluoro-ethanol in 0.5 mL 1,4-dioxane are added 34 mg (0.10 mmol) 2-[4-(2-chloro-pyrimidin-5-ylethynyl)-phenyl]-N-ethyl-propionamide (XVIII.1) in 1 mL 1,4-dioxane, followed by 12 mg (0.30 mmol) sodium hydride (60% in mineral oil). The mixture is stirred at rt for 12 h. After that time, the solvent is evaporated and the residue s purified by HPLC (preparative column: Sunfire, eluent A: water+0.1% TFA, eluent B: MeOH) to yield the desired product.

出典