2-Methylimidazole → Alprazolam

Participants

Reaction Conditions

Reaction Steps

A mixture of 2.8 parts of 7-chloro-2-hydrazino-5-phenyl-3H-1,4-benzodiazepine, 2.8 parts of acetamidine hydrochloride and 2.5 parts of 2-methylimidazole is fused under heating at 160° C for 10 minutes. Water is added to the mixture, followed by extraction with methylene chloride. The methylene chloride layer is washed with water and dried over sodium sulfate. The solvent is evaporated, whereby 8-chloro-1-methyl-6-phenyl-4H-s-triazolo [4,3-a] [1,4] benzodiazepine is yielded. Recrystallization from ethyl acetate yields colorless needles melting at 223° C to 225° C.

Provenance & Evidence