Reacción #1253199

Ecuación de reacción

(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

Disolventes

pyridine

Condiciones de reacción

Tratamiento posterior

1. 1
   Temperaturathe mixture cooled to 0°
2. 2
   OtroThe solvent is removed
3. 3
   workup.DISSOLUTIONthe residue dissolved in dichloromethane
4. 4
   Lavadowashed with water, saline
5. 5
   Secadodried over magnesium sulfate
6. 6
   Concentraciónconcentrated
7. 7
   OtroThe resulting residue is triturated with ether

Procedimiento

(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.

Fuente