Sulfuric Acid → Ezetimibe

Participants

Reaction Conditions

Reaction Steps

5.0 g (9.6 mmol) (3R,4S)-4-[4-(tert-butyl-dimethyl-silanyl-oxy)-phenyl]-1-(4-fluorophenyl)-3-[(S)-3-(4-fluorophenyl)-3-hydroxypropyl]-azetidin-2-on (XI, R4=TBDMS) was solved in 35 ml 2-propanol and 10 ml 2M sulphuric acid solution is added. The solution is heated at 60-70° C. for 1-2 h, and then it was allowed to cool. The product was crystallized by adding ion-free water. The crystalline product was filtered out and washed with water to neutral.

Provenance & Evidence