OPTICALLY ACTIVE QUINOLINE CARBOXYLIC ACID DERIVATIVE HAVING 7-PYRROLIDINE SUBSTITUENT INDUCING OPTICAL ACTIVITY AND METHOD FOR MANUFACTURING THE SAME

PURPOSE: Provided is a method for manufacturing 4-aminomethyl-4-methyl-3-(Z)-alkoxyamino derivative which has antibacterial effects on both gram positive and negative bacteria so that the derivative is useful for medical purposes. And Its pharmaceutically acceptable salt and its solvate are also pro...

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Bibliographic Details
Main Authors SHIN, JEONG HAN, JIN, YUN HO, LEE, CHI U, KIM, NAM DU, CHOI, DONG RAK, JUNG, YONG HO, LEE, JIN SU, YANG, WANG YONG, YOON, SEONG JUN, KIM, IK HOE, SONG, WAN JIN
Format Patent
LanguageEnglish
Korean
Published 06.04.2001
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:PURPOSE: Provided is a method for manufacturing 4-aminomethyl-4-methyl-3-(Z)-alkoxyamino derivative which has antibacterial effects on both gram positive and negative bacteria so that the derivative is useful for medical purposes. And Its pharmaceutically acceptable salt and its solvate are also provided. CONSTITUTION: A method for producing 4-aminomethyl-4-methyl-3-(Z)-alkoxyamino derivative comprises the following steps of: i) reacting the compound of the formula (3) with ketal compound of the formula (2a) in the presence of acid receptor, for 1-24 hours at 0-150 deg.C, preferably from room temperature to 90 deg.C, to manufacture optically active quinoline carboxylic acid derivative of the formula (4); ii) deketalizing the quinoline carboxylic acid derivative to manufacture pyrrolidinone of the formula (5) at from room temperature to 100 deg.C; and iii) reacting the pyrrolidinone with alkoxylamine in the presence of base at 0-90 deg.C. In the formula (1), Q is C-H, C-F, C-CL, or N. Y is H or NH2. R is a C1-C4 linear or branched alkyl, aryl, or benzyl group. * is an optically pure asymmetric carbon.
Bibliography:Application Number: KR20000024657