Biochimica Opos Spa

Proter S.p.a.

Biochimica Ops Spa

Leone Dall'Asta

Marco Da Col

Irene Resta

Gianfranco Cainelli

Luigi Ratti

Michele Contento

Mauro Panunzio

Achille Umani Ronchi

Eugenio Garegnani

Germano Coppi

Sergio Sandri

Mario Ercole Scevola

The present invention refers to process for the preparation of a tiazoline-azetidinone of formula I ##STR1## which comprises N-protecting in position 1 of (3S,4S)-3-phenylace tamido-4-acetoxy-azetidin-2-one, converting the product thus obtained into the corresponding thioamide and subsequently ciclyzing and deprotecting.

Process for the preparation of a thiazoline-azetidinone

The preparation of a novel crystalline cefaclor and the conversion of such a product to cefaclor monohydrate are described. The new intermediate cefaclor is a particular crystalline form and possesses the same antibiotic properties as cefaclor monohydrate.

Crystalline form of a cephalosporin antibiotic

Process for the preparation of a 3,6'-di-N-Acyl-1-[L-(-)-4-Acylamino-2-hydroxybutyryl] kanamycin A, wherein Acyl is a N-protecting acylating group, which comprises reacting kanamycin A with an aluminum salt in an inert organic solvent, treating the aluminum complex thus obtained with a N-acylating agent end acidifiying the reaction mixture, as such or after having removed the complexing aluminum in basic medium and isolated the 3,6'-di-N-Acyl-kanamycin A, to pH 6, treating the protonated 3,6'-di-N-Acyl-kanamycin A, in form of a salt thereof, with an active derivative of L-(-)-4-Acyl-amino-2-hydroxybutyric acid, wherein Acyl is a N-protecting group preferably identical with that which protects the amino groups in the positions 3 and 6' of kanamycin A, and isolating the product thus obtained by simple correction of the pH.

Process for the preparation of amikacin precursors

Process for the preparation of a 3,6'-di-N-Acyl-1-[L-(-)-4-Acylamino-2-hydroxybutyryl] kanamycin A, wherein Acyl is a N-protecting acylating group, which comprises reacting kanamycin A with an aluminum salt in an inert organic solvent, treating the aluminum complex thus obtained with a N-acylating agent and acidifiying the reaction mixture, as such or after having removed the complexing aluminum in basic medium and isolated the 3,6'-di-N-Acyl-kanamycin A, to pH 6, treating the protonated 3,6'-di-N-Acyl-kanamycin A, in form of a salt thereof, with an active derivative of L-(-)-4-Acyl-amino-2-hydroxybutyric acid, wherein Acyl is a N-protecting group preferably identical with that which protects the amino groups in the positions 3 and 6' of kanamycin A, and isolating the product thus obtained by simple correction of the pH.

There is described the preparation of halogenated .beta.-lactam derivatives by introduction of a chlorine atom in the 3-position of the cephem nucleus starting from a 3-sulfonyloxycephem. Such starting materials are reacted with a chlorine ions donor in a basic medium.

Process for the preparation of halogenated .beta.-lactam compounds

Cefadroxil monohydrate is prepared by solubilizing 7-[D-(-)-.alpha.-benzyloxycarbonylamino-.alpha.-(p-hydroxyphenyl)acetamido ]-3-methyl-3-cephem-4-carboxylic acid by silylation or by salification in an organic solvent, subjecting the solubilized acid in the solvent to catalytic hydrogenation, separating the catalyst from the solution, and adding water to the solution at a pH of about 4 to precipitate cefadroxil monohydrate.

Method for the preparation of monohydrate

Cefatrizine 1,2-propylene glycolate is prepared by reacting p-hydroxyphenylglycine chloride hydrochloride with 7-amino-3-iodomethyl-3-cephem-4-carboxylic acid, and then reacting the thus obtained novel intermediate, 7-[D(-)-.alpha.-amino-.alpha.-(p-hydroxyphenyl)-acetamido]-3-iodomethyl-3- cephem-4-carboxylic acid, with the sodium salt of 1,2,3-triazol-4(5)-thiol in 1,2-propylene glycol. The addition of water to the reaction mixture causes the cefatrizine, 1,2-propylene glycolate to precipate.

Process for the prepartion of cefatrizine 1,2-propylene glycolate

A therapeutic treatment for the athrosis diseases comprising administering by intraarticular route from 1 to 5 ml of an aqueous solution containing from 10 to 50 mg of a diacetyl rhein salt having formula (I): ##STR1## wherein M represents an alkali or an earth alkali metal or the residue of an organic base. The diacetyl rhein salts administered by intraarticular route exhibit higher pharmacological activity than the corresponding diacetylrhein administered orally.

Diacetylrhein salts and their therapeutical use in the treatment of

A process for preparing Tetroxoprim starting from 3,5-dimethoxy-4-methoxyethoxy-benzaldehyde and 2,4-diamino-6-hydroxy-pyrimidine, by successive hydrogenation, halogenation and hydrogenolysis of the 2,4-diamino-6-oxo-5-(3,5-dimethoxy-4-methoxyethoxy-benzylidene)-pyrimidine obtained in the initial reaction.

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Pavia, Italy

Leone Dall'Asta