反応 #1253199

反応方程式

(5R)-3-(3-Fluoro-4-[4-(2-fluoroethyl)-3-oxopiperazin-1-yl]phenyl)-5-hydroxymethyloxazolidin-2-one

Triethylamine

methanesulfonyl chloride

→

(5R)-3-(3-fluoro-4-[4-(2-fluoroethyl)-3-oxopiperazin-1-yl]phenyl)-5-(methanesulfonyloxymethyl)oxazolidin-2-one

溶媒

pyridine

反応条件

後処理

1. 1
   温度the mixture cooled to 0°
2. 2
   その他The solvent is removed
3. 3
   workup.DISSOLUTIONthe residue dissolved in dichloromethane
4. 4
   洗浄washed with water, saline
5. 5
   乾燥dried over magnesium sulfate
6. 6
   濃縮concentrated
7. 7
   その他The resulting residue is triturated with ether

実験手順

(5R)-3-(3-Fluoro-4-[4-(2-fluoroethyl)-3-oxopiperazin-1-yl]phenyl)-5-hydroxymethyloxazolidin-2-one (0.8 g) is dissolved in pyridine (15 ml) and the mixture cooled to 0°. Triethylamine (0.38 ml) and methanesulfonyl chloride (0.19 ml) are added to the mixture, and stirring continued at 20-25° for 2 hours. The solvent is removed and the residue dissolved in dichloromethane, washed with water, saline, dried over magnesium sulfate and concentrated. The resulting residue is triturated with ether to give (5R)-3-(3-fluoro-4-[4-(2-fluoroethyl)-3-oxopiperazin-1-yl]phenyl)-5-(methanesulfonyloxymethyl)oxazolidin-2-one (0.76 g) which is used without further purification.

出典