Process for the preparation of quinoline carboxylic acids

Details Process for the preparation of quinoline carboxylic acids Process for the preparation of quinoline carboxylic acids

1989-01-10

1991-01-01

Raymond, Richard L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544363, 546 13, C07D24104

Patent

active

049819666

ABSTRACT:
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.

REFERENCES:
patent: 4528287 (1985-07-01), Itoh et al.
patent: 4806645 (1989-02-01), Hermecz et al.
"Chemical Abstracts", vol. 103, 1985, Col. 103:123491p. (Abstract of Japanese Patent No. 60-78,986, pub. 5/4/85).
"Chemical Abstracts", vol. 105, 1986, Col. 105:153293j, (Abstract of Japanese Patent No. 60-75,489, pub. 4/27/85).

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