1 results about "Marbofloxacin" patented technology

This invention discloses a mabofloxacin intermediate, belonging to the field of drug synthesis technology. First, aminomethylamine and methyl formate are condensed at low temperature to generate MBX-1. Then, a fluoroquinolone core is constructed using a stepwise process of high-temperature acylation condensation, low-temperature nucleophilic substitution, and intermediate-temperature cyclization to obtain MBX-6. Next, in an optimized toluene system, N-methylpiperazine is introduced into the core via high-temperature nucleophilic substitution. After multi-step purification, MBX-7 is obtained. Finally, the quinolone skeleton is reconstructed through an integrated alkaline hydrolysis-acid-catalyzed cyclization process, followed by temperature-controlled recrystallization purification to obtain mabofloxacin intermediate MBX-9. This invention achieves high-purity, low-residue, and high-yield preparation of mabofloxacin intermediates by establishing a DMF-free green solvent system and a precise temperature control strategy. This effectively solves the industrialization problems of excessive residues, increased side reaction impurities, and low overall yield caused by the use of hazardous solvents in existing technologies.