| 摘要 |
PURPOSE: Provided is a method for manufacturing ethyl 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoyl acetate more easily in a high yield without using column chromatography. The compound is used in manufacturing Levofloxacin, as an intermediate. CONSTITUTION: Ethyl 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoyl acetate is manufactured by the following steps of: i) reacting 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoic acid of the formula (2) with thionyl chloride used as solvent at 20-150 deg.C, preferably 60-80 deg.C, for 2-20 hours, preferably 4-6 hours, to obtain 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoyl chloride of the formula (3); and ii) reacting 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoyl chloride of the formula (3) with magnesium malonate of the formula (4) under alkaline solution at minus10-100 deg.C, preferably 20-30 deg,C, for 2-50 hours, preferably 24-28 hours, to obtain ethyl 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoyl acetate of the formula (1).
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