Archifar Industrie Chimiche Del Trentino S.p.a.

Archifar Laboratori Chimico Farmacologici S.p.a.

Archifar Laboratori Chimico Farmachologici S.p.a.

Archifar Laboratori Chimice Farmacologici S.p.a.

Carmine Pasqualucci

Leonardo Marsili

Vittorio Rossetti

Giovanni Bonfanti

Pietro Cesti

Giuseppe Scarpitta

Method of producing derivatives of 6-.beta.-amidinopenicillanic acid, according to which a derivative of 6-aminopenicillanic acid is condensed with a reactive derivative of disubstituted amide in an inert anhydrous solvent and in the presence of a tertiary amine. In such a reaction, the reactive derivative of the disubstituted amide comprises a complex of an amide of carboxylic acid.

Method of producing derivatives of 6-.beta.-amidinopenicillanic acid

Novel rifamycin compounds of high antibiotic activity. Such compounds are obtained by reacting 3-amino-4-deoxo-4-imino-rifamycin S with aldehydes.

Novel rifamycin compounds of high antibiotic activity

Oxidized rifamycin compounds having high antibiotic activity as obtained by reacting 3-amino-4-deoxo-4-imino-rifamycin S or related compounds with a ketone.

Rifamycin compounds

3-nitro-rifamycins S and SV useful as starting compounds for the production of antibiotic substances. Such compounds are obtained by reaction of a 3-bromo-rifamycin S with sodium nitrite in a dipolar aprotic solvent at a temperature from room temperature to +40.degree. C.

3-Nitro-rifamycins S and SV

Method of preparing 3-amino-rifamycins S and SV having antibiotic activity. According to such a method a 3-bromo-rifamycin S is reacted with sodium nitrite to give 3-nitro-rifamycin S which is reduced with zinc powder to give the 3-amino-rifamycin SV from which the 3-amino-rifamycin S can be obtained by treatment with an oxidating agent.

Process for producing 3-amino-rifamycins S and SV

Rifamycin compounds having high antibacterial activity, consisting of powder colored from yellow to orange. Such compounds are provided by reacting 3-amino-rifamycin S with an aldehyde of formula X--CHO in the presence of a reducing agent and in an organic solvent.

Rifamycin compounds having high antibacterial activity, comprising derivatives of 3-aminosubstituted-4-desoxo-4-imino rifamycin S. These compounds are powders of red violet color and are provided by reacting 3-aminosubstituted rifamycin S with ammonia gas.

Rifamycin compounds having high antibacterial activity, comprising powder of yellow-orange color. Such compounds are obtained by reacting 3-aminosubstituted-4-desoxo-4-imino rifamycin S with aldehydes of formula X--CHO.

Rifamycin compounds having high antibacterial activity, comprising powders of red-violet color. Such compounds are obtained by reacting 3-aminosubstituted-4-desoxo-4-imino rifamycin S with linear and cyclic ketones.

Novel rifamycin compounds having high antibiotic activity. Such compounds are obtained by reacting 3-amino-rifamycin SV with an aldehyde, particularly a heterocyclic aldehyde.

Novel rifamycin compounds having high antibiotic activity. Such compounds are obtained by reacting 3-amino-rifamycin SV with an aldehyde, particularly an aliphatic or cycloaliphatic aldehyde.

Rifamycin compounds having high antibacterial activity, comprising red-orange powders. Such compounds are provided by reacting 3-bromo-rifamycin S with a compound having the formula H.sub.2 N--CS--NH--X.

Oxidized rifamycin compounds having high antibiotic activity as obtained by reacting 3-amino-4-deoxo-4-imino-3-rifamycin S or homologous thereof with a ketone.

Rifamycin compounds having high antibiotic activity, comprising rose-colored powders, water insoluble, but soluble in most of the organic solvents. Such compounds are obtained by reacting 3-amino-rifamycin S with gaseous ammonia in ethers and/or aromatic hydrocarbons at a temperature between 0.degree. C and +30.degree. C, stirring the mixture for at least 3 hours, and then isolating the compound thus obtained.

Method of preparing 3-amino-Rifamycin S and 3-azido-Rifamycin S and 25-desacetyl derivatives thereof having antibiotic activity. According to such a method, Rifamycin S is dissolved in dipolar aprotic solvent and reacted with sodium azide.

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Milan, Italy

Carmine Pasqualucci