Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

Peter Ritli

Istvan Hermecz

Agnes Horvath

Judit Sipos

Aniko Pajor

Geza Kereszturi

Maria Balogh

Gabor Kovacs

Lelle Vasvari

Tamas Szuts

Katalin Marmarosi

Lelle V Vasvari Nee Debreczy

Zoltan Meszaros, Deceased

Lelle Vasvavi

Marie Balogh

Maria Halogh

Geza Keresturi

Lelle V Debreczy

The invention relates to a new process for the preparation of antibacterial compounds of the Formula I ##STR1## wherein R.sup.1 stands for phenyl substituted by 1 or 2 halogen atoms;

Process for the preparation of quinoline carboxylic acid derivatives

The invention relates to a new process for the preparation of compounds of the general Formula I ##STR1## wherein R stands for piperazinyl, 4-methyl-piperazinyl or 4-ethyl-piperazinyl group and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II ##STR2## wherein R.sup.1 and R.sup.2 stand for halogen, for an aliphatic acyloxy group containing 2 to 6 carbon atoms and optionally substituted by halogen, or for an aromatic acyloxy group containing 7 to 11 carbon atoms with a piperazine derivative of the general Formula III ##STR3## wherein R.sup.3 stands for hydrogen, methyl or ethyl or a salt thereof and subjecting the compound of the general Formula IV ##STR4## thus obtained wherein R, R.sup.1 and R.sup.2 are as stated above to hydrolysis after or without isolation and if desired converting the compound of the general Formula I thus obtained into a salt thereof or setting free the same from its salt. The compounds of the general Formula I are known antibacterial agents.

Process for the preparation of quinoline carboxylic acids

The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen: or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt. The compounds of the Formula I are known antibacterial agents.

A method of using a compound of the Formula (V) ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, wherein R.sup.1 and R.sup.2 are each C.sub.1 to C.sub.6 aliphatic acyloxy, unsubstituted or substituted by halogen, or are each C.sub.7 to C.sub.11 aromatic acyloxy, for preventing amination of the 6-position when a compound of the Formula (I) ##STR2## or a pharmaceutically acceptable salt thereof is to be formed, which comprises the steps of:

Process for the preparation of quinoline carboxyolic acids

Baron chelates of quinoline carboxylic acids

The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt. The compounds of the Formula I are known antibacterial agents. The advantage of the process of the present invention is that it makes the desired compounds of the Formula I available in a simple manner, with high yields and in a short reaction time.

Quinoline carboxylic acid boric acid anhydrides

1-Methylamino-quinoline-carboxylic acid derivatives

Boric anhydrides of

Norfloxacin intermediate

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Budapest, Hungary

Peter Ritli