PROCESS FOR PREPARATION OF ALKYL 2-(2,3,5-TRIFLUORO-4-(4-METHYL-1-PIPERAZINYL)) BENZOYL-3(S)-(1-HYDROXYPROP-2-YLAMINO) ACRYLATE

摘要

PURPOSE: Provided is a process for the preparation of alkyl 2-(2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)) benzoyl-3(S)-(1-hydroxyprop-2-ylamino) acrylate which has an optical activity and is thus used as an intermediate in manufacturing Levofloxacin. CONSTITUTION: Alkyl 2-(2,3,5-trifluoro-4-(4-methyl-1-piperazinyl)) benzoyl-3(S)-(1-hydroxyprop-2-ylamino) acrylate is represented by the formula(1), wherein R is C1-C4 alkyl group and manufactured by reacting a compound for the formula(5) with a compound for the formula(4) in the presence of protic polar solvent at 0-100 deg.C. Where, the compound of the formula(5) is manufactured by reacting a compound of the formula(20 with a formula(3) in polar solvent at -5 to 100 deg.C.