113933-55-4

Upstream product

• 94695-48-4 2,3,4,5-tetrafluorobenzoyl chloride 
• 924-99-2 ethyl 3-(dimethylamino)acrylate 
• 108860-30-6 ethyl 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)-benzoyl acetate 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 

Downstream Products

• 106017-08-7 Rufloxacin hydrochloride 
• 100986-85-4 levofloxacin 
• 177472-30-9 C₂₀H₂₄FN₃O₄ 
• 177472-28-5 (S)-ethyl 3-(1-hydroxypropan-2-ylamino)-2-(2,3,5-trifluoro-4-(4-methylpiperazin-1-yl)benzoyl)acrylate 
• 138944-12-4 ethyl 2-<2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)-benzoyl>-3-(1-mercaptoeth-2-ylamino)-acrylate 

Relevant academic research and scientific papers

Preparation method of levofloxacin and intermediates thereof

The invention relates to a preparation method of levofloxacin and intermediates thereof, and belongs to the field of medicinal chemistry. The preparation method comprises the following steps of: carrying out amino substitution and ring closing reaction on a fluorine-substituted substrate to integrate a plurality of intermediates into a one-pot reaction, and hydrolyzing under acidic conditions to obtain levofloxacin. According to the method, the reaction operation is simplified, the production period is greatly shortened, multiple times of after-treatment are not needed, emission of three wastes is reduced, the method is more environmentally friendly, the reaction yield is increased by about 20% compared with the prior art, and the method is suitable for industrial amplification.

One-pot synthesis of rufloxacin

Rufloxacin (MF-934) was prepared in one-pot synthesis in 61% yield by treatment of the 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)-benzoyl acetate, first with N,N-dimethylformamide dimethyl acetal, then with 2-aminoethanethiol, followed by cyclization and