2-Methylpiperazine → Gatifloxacin

Participants

Reaction Conditions

Reaction Steps

Thirty five grams of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid and 24.9 g (2.1 eq) of 2-methyl piperazine were put in suspension in DMSO (700 mL) under nitrogen atmosphere. The mixture was heated to 55° C. during 24 hours. The reaction mixture was then stirred at 20° C. overnight. Half of this solution (408 g, assay 4.8%) was filtrated and dried under vacuum to obtain 15.0 g (66% yield) of gatifloxacin.

Provenance & Evidence