2-Methylpiperazine → Gatifloxacin

Participants

Reaction Conditions

Reaction Steps

Forty grams of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid and 28.4 g (2.1 eq) of 2-methyl piperazine were put in suspension in DMSO (800 mL) under nitrogen atmosphere. The mixture was heated to 55° C. during 24 hours. Subsequently, the mixture was heated to 70° C. and half of the amount of DMSO was distilled-off at reduced pressure (1-5 mm Hg). At the end of the distillation, toluene (200 mL) was added, the reaction mixture was cooled to 5° C., and held at this temperature overnight. The solution was filtered and dried under vacuum to obtain 38 g after assay (75% yield) of gatifloxacin.

Provenance & Evidence