Bayer Aktiengesellschaft

Rudolf Zerbes

Karl H Mohrmann

Siegfried W Linke

Wolf Reiser

Paul Naab

Erik Regel

Gerhard Franckowiak

Michael Preiss

Herbert Diehl

Ulrich Schorsch

Arthur Haaf

The present invention relates to a one-pot process for the preparation of 7-heterocyclyl-substituted 3-quinolonecarboxylic acid derivatives. They possess a strong anti-microbial effect. They include active compounds such as, for example, ofloxacin, ciprofloxacin or enrofloxacin.

One-pot process for the preparation of 3-quinolonecarboxylic acid

A process for the preparation of an oxirane of the formula ##STR1## in which Y is chlorine or phenyl,

Preparation of oxiranes

Known quinolone carboxylic acid derivatives of the formula ##STR1## are treated so as to become readily administrable parenterally, the treatment comprising dissolving the active compound using an acid, allowing the solution to stand for about 0.15 to 150 hours at a temperature from room temperature to the boiling point of the solution, filtering the solution, precipitating the active compound from the solution using a basic reagent, and converting the precipitated active compound into a form which can be administered parenterally.

Process for the preparation of quinolonecarboxylic acids which can be

A process for the preparation of oxiranes is disclosed in which a ketone of the formula ##STR1## wherein Y represents chlorine or phenyl, X represents oxygen or CH.sub.2 and Z represents hydrogen or halogen is reacted with trimethylsulphonium methyl sulphate formed by treating dimethyl sulphide with dimethyl sulphate. The process is carried out in the presence of potassium hydroxide or sodium hydroxide powder in an inert organic diluent at 0.degree. to 60.degree. C. The products are useful as intermediates for the formation of plant growth regulants and fungicides.

Process for the preparation of oxiranes

A process for the preparation of oxiranes is disclosed in which trimethylsulphonium methyl sulphate, formed by treating dimethyl sulphide with dimethyl sulphate in the presence of tert.-butanol, is reacted, without previous isolation, with a ketone in the presence of a base and in the presence of tert.-butanol. The resultant oxiranes are useful in the preparation of plant growth regulants and fungicides.

Imidazolyl-methane derivatives of the formula ##STR1## where Ar is an optionally substituted phenyl and R.sup.1 is alkyl or optionally substituted phenyl is prepared by reaction of a ketone of the formula

Process for the preparation of imidazolyl-methane derivatives

A process for the preparation of an oxirane of the formula ##STR1## in which Y represents chlorine or phenyl, X represents oxygen or Ch.sub.2 and Z represents hydrogen or halogen, which comprises containing dimethyl sulphoxide with dimethyl sulphate whereby to form trimethyloxosulphonium methyl sulphate of the formula

A process has been developed for the recovery of (1-S)-2-oxo-bornane sulphonic acid (D-camphor-.beta.-sulphonic acid) from contaminated aqueous solutions, particularly from those which arise as mother liquors from the resolution of the racemates of amino compounds wherein said solutions are treated with guanidine bases (or soluble salts thereof) of the formula ##STR1## in which Ar is an optionally substituted aryl radical at pH about 3.5 to 7.5 and the guanidinium camphorsulphonate is separated off and split. The process is effective even where the mother liquors are contaminated with large amounts of inorganic salts.

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Wuppertal, Germany

Rudolf Zerbes