Plurichemie Anstalt

Hovione Inter Limited

Plurichenue Anstalt

Philip R Page

Ivan Villax

William Heggie

Michael B Hursthouse

Indira Ghatak

Richard Somerville

A process for the preparation of .mu.-3-carbopentazane-N.sup.1, N.sup.4 :N.sup.2, N.sup.5 -bis-[bis(triphenylphosphine)rhodium (I)] dinitrate by the reaction of tris(triphenylphosphine)nitratorhodium (I) with hydrazine in degassed methanol under an inert atmosphere.

Process for the preparation of a rhodium complex

Novel esters of 9.alpha.-fluoro- and chloro-corticosteroids of the formula ##STR1## wherein Y is chlorine or OR.sub.1, R.sub.1 and R.sub.2 represent an acyl group of 2-6 carbon atoms or a benzoyl group and where R.sub.1 and R.sub.2 can be the same or different in the same molecule, R.sub.3 is methyl or fluorine in either the .alpha.- or .beta.- orientation, X is chlorine or fluorine, and the C.sub.1  C.sub.2 bond can be saturated or not, especially those compounds of the formula ##STR2## wherein Y and R.sub.2 have the significance given above, are prepared by reacting the respective 9.beta.,11.beta.-epoxy compounds with hydrogen fluoride or chloride.

Novel 9.alpha.-fluoro- or chloro-corticosteroid esters and a process for

The present invention refers to the compounds (.mu.-hydrazine-N.sup.1 :N.sup.2)-bis[bis(triphenylphosphine)-chlororhodium (I)] and di(.mu.-hydrazine-N.sup.1 :N.sup.2)-bis[bis(triphenylphosphine)rhodium (I)] dichloride, which are homogenous hydrogenation catalysts and their application in the hydrogenation of the exocyclic methylene group of acid addition salts of 6-demethyl-6-deoxy-6-methylene-5-hydroxytetracycline (methacycline) to prepare .alpha.-6-deoxy-5-hydroxytetracycline (doxycycline).

Preparation of a new catalyst containing rhodium

Preparation of novel solvates of beclomethasone 17,21-dipropionate, by dissolution of beclomethasone 17,21-dipropionate in an ethereal or halogenated hydrocarbon solvent and precipitation by the addition of di-isopropyl ether. These new solvates are bulk stable, in both the micronized and non-micronized forms. The micronized form is especially suitable for the preparation of stable aerosol.

Preparation and use of new solvates of beclomethasone 17,21-dipropionate

The present invention refers to complexes prepared by reacting rhodium trinitrate with a suitable hydrazine and a suitable tertiary phosphine, more specifically to the compounds di(.mu.-hydrazine-N.sup.1 :N.sup.2)-bis[bis(triphenylphosphine)rhodium (I)]dinitrate and .mu.-3-carbopentazane-N.sup.1, N.sup.4 :N.sup.2, N.sup.5 -bis[bis(triphenylphosphine)rhodium (I)]dinitrate, which are homogenous hydrogenation catalysts and their application in the hydrogenation of the exocyclic methylene group of acid addition salts of 6-demethyl-6-deoxy-6-methylene-5-hydroxytetracycline (methacycline) to prepare .alpha.-6-deoxy-5-hydroxy-tetracycline (doxycycline).

Process of preparation of novel rhodium hydrogenation catalysts

A homogenous hydrogenation process of preparing 6-demethyl-6-deoxy-6 methylene-5-hydroxytetracycline using a stereospecific tertiary phosphine-hydrozino-rhodium complex catalyst.

New process for the preparation of alpha-6-deoxy-5-hydroxytetracycline

Application of catalysts containing rhodium

The present invention refers to complexes prepared by reacting rhodium trinitrate with a suitable hydrazine and a suitable tertiary phosphine, more specifically to the compounds di(.mu.-hydrazine-N.sup.1 :N.sup.2)-bis[bis(triphenylphosphine)rhodium (I)]dinitrate and .mu.-3-carbopentazane-N.sup.1,N.sup.4 :N.sup.2,N.sup.5 -bis[bis(triphenylphosphine)rhodium (I)]dinitrate, which are homogeneous hydrogenation catalysts and their application in the hydrogenation of the exocyclic methylene group of acid addition salts of 6-demethyl-6-deoxy-6-methylene-5-hydroxytetracycline (methacycline) to prepare .alpha.-6-deoxy-5-hydroxy-tetracycline (doxycycline).

Process of preparation of novel rhodium hydrogenation catalysts and

A homogeneous stereospecific rhodium complex hydrogenation catalyst is prepared using a degassed organic solvent and eventually water.

Homogeneous catalytic system and a process for the preparation of same

A process for the preparation of corticosteriod esters of the formula ##STR1## in which ---- signifies that a double bond can be present;

Novel process for the preparation of steroidal esters

A process for the preparation of .alpha.-6-deoxy-tetracyclines by the stereoselective heterogeneous hydrogenation of a 6-demethyl-6-deoxy-6-methylene-tetracycline or an acid addition salt thereof, in the presence of a tertiary phosphine, or the simultaneous dehalogenation and stereo-selective heterogeneous hydrogenation of an 11a-halo-6-demethyl-6-deoxy-6-methylene-tetracycline or an acid addition salt thereof, in the presence of a tertiary phosphine, characterized by the use of a rhodium salt catalysts, wherein the rhodium is bonded to a polysiloxane carrier, having the following formulae:

Process for the preparation of .alpha.-6-deoxy-tetracyclines

Stable homogeneous hydrogenation catalysts are prepared by reacting a rhodium salt or complex with a hydrazine in the presence or absence of a tertiary phosphine.

Homogeneous catalytic system comprising rhodium, hydrazine and phosphine

An improved process for the preparation of .alpha.-6-deoxytetracyclines and more particularly to the stereo specific hydrogenation of the 6-methylene group of 6-deoxy-6-demethyl-6-methylene-5-hydroxytetracyline and of its 11a-halo-analog, is described in which the catalyst is the reaction product of a rhodium salt or a complex with a hydrazine or salt thereof.

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

The 17.alpha.-monoesters and 17.alpha.,21-diesters of corticosteriods are well known and represent nowadays the most efficient group of anti-inflammatory compounds for topical application, having minimal systemic action.

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Sintra, Portugal

Philip R Page