The invention discloses a one-pot method for green and efficient preparation of
marbofloxacin, and the method comprises the following steps: carrying out
hydrolysis reaction on 6, 8-difluoro-1-(methylamino)-7-(4-methylpiperazine-1-yl)-4-oxo-1, 4-dihydroquinoline-3-
carboxylic acid (a substrate I) to prepare an intermediate I; the intermediate I is cyclized to obtain
marbofloxacin, a main alkali and auxiliary alkali compounded
system is adopted in the
hydrolysis reaction, the main alkali is
sodium hydroxide or
potassium hydroxide, and the auxiliary alkali is
tetrasodium iminodisuccinate. A KOH / IDS-Na
compound system is adopted, the
reaction conditions are mild, the reaction time is short, the consumption is small, and the severe conditions that a large amount of
tetramethylammonium hydroxide is used and the temperature is high in the literature can be avoided. In the cyclization reaction, an HCl /
paraformaldehyde system is adopted, so that the problem of nonuniformity of a
formaldehyde aqueous solution in production operation can be avoided; the
marbofloxacin is directly and greenly synthesized under mild conditions, the marbofloxacin can be obtained only through simple
filtration subsequently, the yield is effectively improved, energy is saved, waste is reduced, the production cost is greatly reduced, and the method is suitable for industrial production.