Dobfar S.p.a.

Ankerfarm, S.p.a.

Renato Broggi

Marco Falciani

Leonardo Marsili

Gino Cotti

There are provided 3-azinomethyl rifamycins of the formula I: ##STR1## wherein R represents hydrogen or acetyl;

3-azinomethyl rifamycins

Cephapirine esters having the formula ##STR1## wherein R is selected from the group consisting of ##STR2## Such esters and salts thereof, having antibiotic activity, are prepared by reacting 7-ACA with bromophtalide or chloromethylpivalate in the presence of an alkylamine, at a temperature in the range of 0.degree.-70.degree. C. The reaction compound is reacted with chlorohydrate chloride of 4-piridylthioacetic acid. A salt of the compound of formula (I) is isolated from the reaction mixture, after washing with acidic water and addition of a pharmaceutically acceptable acid, by treatment with a suitable solvent.

Cephapirine esters and salts thereof

Cephalosporine desacetoxy esters having the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and R.sub.1 is selected from the group consisting of ##STR3## Such esters and salts thereof having antibiotic activity are prepared by reacting 7-ADCA with bromophthalide or chloromethyl pivalate in the presence of an alkylamine at a temperature in the range of 0.degree.-70.degree. C. The reaction product is reacted with chloride chlorohydrate of D(-)dihydrophenylglycine or D(-)p-hydroxy phenylgycine. A salt of the compound of formula (I) is isolated from the reaction mixture, which after washing with acidic water and addition of a pharmaceutically acceptable acid is obtained by treatment with suitable solvent.

Cephalosporine desacetoxy esters and salts thereof

N-carboxy cefadroxil disodium salt having formula ##STR1## Said salt is endowed with antibiotic activity and can be administered parenterally.

N-Carboxy cefadroxil sodium salt

Salts of cefadroxil with an amino acid selected from the group consisting of L-lysine, L-arginine and acetylcysteine. Said salts are obtained by reacting an aqueous suspension of cefadroxil with an aqueous solution of an amino acid or its derivative, selected from the group consisting of L-lysine, L-arginine and acetylcysteine. To isolate the salt, the aqueous solution is submitted to lyophilization.

Cefadroxil acetylcysteinate salt

Process for the production of 6-D-.alpha.-amino-p-hydroxyphenylacetamido penicillanic acid which is a potent antibiotic also known generically as amoxicillin. According to the process there is reacted a boron derivative of 6-APA with an acylating agent derived from the D(-)-p-hydroxyphenylglycine, in dimethylformamide or in dimethylsulfoxide in admixture with methylene chloride or chloroform, hydrolyzing and then removing the enaminic group.

Process for the production of 6-D-.alpha.-amino-p-hydroxyphenylacetamido

Process for preparing cephalexine monohydrate and cephadroxyl monohydrate, according to which a reaction is carried out of a mixed anhydride prepared from a Dane salt of phenylglycine or p-hydroxyphenyl-glycine with a chloroformiate, with an aqueous solution of 7-ADCA in a solvent selected from the group comprising dimethyl sulphoxide, dimethylacetamide, formamide, dimethylformamide and dioxane.

Process for preparing derivatives of 7-amino-desacetoxy cephalosporanic

A process is provided for preparing alpha-6-deoxytetracyclines depicted by the formula: ##STR1## wherein Y is H, F, Cl, Br or I; and R is H, OH or --O--CO--(C.sub.1-6 alkyl); which comprises: contacting a 6-demethyl-6-deoxy-6-methylene tetracycline or salt thereof having the formula ##STR2## in which Y and R are as given above, with hydrogen at a temperature of between 15.degree. C. and 80.degree. C. in the presence of a catalyst soluble in a polar solvent, said catalyst being a complex of rhodium with electron donor ligands of a tertiary phosphine selected from the group consisting of triphenylphosphine, tributylphosphine, triethylphosphine, diethylphenylphosphine and diphenylethylphosphine and said polar solvent being a mono- or polyhydric alcohol with from 1 to 4 carbon atoms, N,N-dimethylformamide, N,N-dimethylacetamide, dioxan, tetrahydrofuran, methoxyethanol, ethoxyethanol, acetonitrile or pyridine.

Process for the preparatin of .alpha.-6-deoxytetracyclines

A process for preparing cephalosporines in which a cephalosporanic derivative is treated with a polar solvent, then with an organic base to give a mixture which is cooled at a temperature lower than -25.degree. C. A cyclic derivative of boron is added to the mixture and the temperature is increased to about 0.degree. C. An intermediate compound is formed which by treatment first with an acylating agent and then with a mixture of water and alcohol provides a solution containing cephalosporines.

Process for preparing cephalosporines

A process for preparing penicillins, in which 6APA is treated with a polar solvent, then with an organic base to give a mixture which is cooled at a temperature lower than -25.degree. C. A cyclic derivative of boron is added to the mixture and the temperature is increased to about 0.degree. C. An intermediate compound is formed which by treatment first with an acylating agent and then with a mixture of water and alcohol provides a solution containing the penicillin.

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Milan, Italy

Renato Broggi