| 摘要 |
PURPOSE: Provided is a method for manufacturing ethyl 2-£2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)|benzoyl-3(S)-(1-hydroxyprophy-2-nilamino) acrylate more easily in a high yield. The compound is used in manufacturing an antibacterial agent, Levofloxacin, as an intermediate. CONSTITUTION: Ethyl 2-£2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)|benzoyl-3(S)-(1-hydroxyprophy-2-nilamino) acrylate represented by the formula (1) is manufactured by the following steps of: i) reacting ethyl 2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)benzoyl acetate of the formula (2) with triethyl orthoformate of the formula (3) under a nonpolar solvent at 20-200 deg.C, preferably 100-120 deg.C, for 2-50 hours, preferably 22-28 hours, to obtain an intermediate of the formula (4); and ii) reacting the intermediate of the formula (4) with (S)-(+)-2-amino-1-propanol having optical activity under a polar solvent at 0-100 deg.C, preferably 10-30 deg.C, for1-10 hours, preferably 2-3 hours, to obtain ethyl 2-£2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)|benzoyl-3(S)-(1-hydroxyprophy-2-nilamino) acrylate.
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