Réaction #76815

Équation de réaction

Benzoyl chloride

pregabalin

→

4

Rendement 47.0%

(S)-3-(Benzoylaminomethyl)-5-methylhexanoic Acid

Rendement 47.0%

Solvants

THF

Conditions de réaction

Traitement

1. 1
   FiltrationThe reaction mixture was then filtered
2. 2
   Concentrationconcentrated in vacuo
3. 3
   AutreThe residue was chromatographed (SiO2, heptane-ethyl acetate, 1:1 to 3:7)

Mode opératoire

Benzoyl chloride (0.88 ml, 7.6 mmol) was added to a stirred suspension of pregabalin (1.0 g, 6.3 mmol) in THF (80 ml) at room temperature under argon and the reaction mixture was stirred for 18 hours. The reaction mixture was then filtered and concentrated in vacuo. The residue was chromatographed (SiO2, heptane-ethyl acetate, 1:1 to 3:7) to give 4 (0.78 g, 47%).

Source