Abstract: A process for preparing compounds of formula [II] by esterification of the C-17 hydroxyl group of 6?,9?-difluoro-11?,17?-dihydroxy-16?-methyl-3-oxoandrosta-1,4-diene-17?-carbothioic acid, the compound of formula [I] comprises treating compound [I] with a slight excess of an acyl chloride of general formula R—COCl, where R represents —CH2CH3, —CH2CH2CH3 or —CH(CH3)2, in an inert solvent, in the presence of a tertiary amine. Preferably the process is carried out using pyridine in the presence of acetone at a temperature of from 5° C. to ?20° C.

Abstract: The present invention provides electrophilic alkylating reagents of formula II, wherein is an aryl group, R2 is an alkyl group, R3 is a substituted phenyl group, wherein the number of substituents (n) is greater than 2 and R4 is an anion, and salts thereof, methods for their preparation and methods for the preparation of alkylated biologically active compounds using such reagents.

Abstract: Described is a process for the preparation of monofluoromethylated organic biologically active compounds using monofluoromethylated reagents. Fluticasone Propionate and Fluticasone Furoate can be prepared using, for example, S-monofluoromethyl-S-phenyl-2,3,4,5-tetramethylphenylsulfonium tetrafluoroborate as monofluoromethylating reagent instead of bromofluoromethane.

Abstract: A process for reducing the particle size of an active pharmaceutical ingredient (API) while maintaining its polymorphic form, comprises the step of processing the active pharmaceutical ingredient by cavitation at elevated pressure. The process preferably comprises the step of isolating the processed active ingredient in the form of powder, wherein the isolation step comprises filtration or spray drying. Particles produced by the process of the invention typically have a span value of less than 2.5.

Abstract: Particles containing a tetracycline or one of its pharmaceutically acceptable salts and an antioxidant, formulations containing the same and their use in the treatment of infectious diseases are described. Methods of encapsulation of a tetracycline or one of its pharmaceutically acceptable salts and an antioxidant are also disclosed.

Abstract: Described are processes for the preparation of monofluoromethylated organic biologically active compounds, such as Fluticasone Propionate and Fluticasone Furoate, in the presence of fluorodecarboxylating reagents such as XeF2 and BrF3.

Abstract: A process for producing tamsulosin of formula I and pharmaceutically acceptable addition salts, thereof comprises the steps of: a) Reacting compound R,R-[2-(4-methoxy-phenyl)-1-methyl-ethyl]-(1-phenyl-ethyl)-amine of formula II or a salt thereof ?with chlorosulfonic acid with or without an organic solvent, to obtain compound R,R-2-methoxy-5-[2-(1-phenyl-ethylamino)-propyl]-benzenesulfonic acid of formula III b) Hydrogenolysis of compound R,R-2-methoxy-5-[2-(1-phenyl-ethylamino)-propyl]-benzenesulfonic acid of formula III or a salt thereof carried out in an alcohol in the presence of a palladium catalyst using hydrogen or a source of hydrogen, to obtain compound R-(?)-5-(2-amino-propyl)-2-methoxy-benzenesulfonic acid of formula IV c) Reacting primary amine R-(?)-5-(2-amino-propyl)-2-methoxy-benzenesulfonic acid of formula IV, or a salt thereof, with a compound of formula V ?wherein X represents an halogen atom selected from the group consisting of Cl; Br and I, to obtain 5-{(2R)-2-

Abstract: A process for the production of iohexol comprises alkylating 5-Acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide using 2(2-methoxy-ethoxy)-ethanol as solvent in the presence of a base, and optionally isolating crude iohexol from the reaction mixture. Preferably, the alkylating agent is 1-chloro-2,3 propanediol and the base is an alkali metal hydroxide such as sodium hydroxide or potassium hydroxide.

Abstract: The object of the present invention is an industrial process for the purification and removal of residual solvents from iohexol, based on the suspension of crystalline iohexol, eventually containing residual solvents above 100 ppm, in a fluid wherein it has a low solubility, followed by heating, filtration and drying. The process allows the formation of crystalline iohexol with no residual organic residual solvent above 100 ppm and with an increased purity level.

Abstract: A process for the purification of roxithromycin, an antibiotic for therapeutic purposes, in which the purification is carried out by the dissolution or suspension of the product in methanol followed by cooling. Purification may also be obtained by addition of a non-solvent and/or by concentration of the mixture, thus obtaining a purified product.

Abstract: The invention provides a new process for the preparation of mometasone 17-furoate, a steroid derivative useful in the treatment of inflammatory disease, by direct esterification of the 17 hydroxyl group without prior protection of the free 11 hydroxy function.

Abstract: The present invention refers to a process for the preparation of 4-(des-dimethylamino)-tetracyclines, which compounds have a therapeutical application. The starting tetracyclines are treated with a methylating agent and the resulting trimethylammonium salts are reduced by electrolysis in an aqueous solution at acidic pH, in the presence of an adequate electrolyte. A direct electrical current with a potential of 0.5-1.5 volts is applied between two convenient electrodes until the reaction is complete. The 4-(des-dimethylamino)-tetracyclines are isolated by extraction with an organic solvent.

Abstract: The present invention describes a new process for the preparation of azithromycin from a suitable imino ether as precursor, characterised by the fact that the reduction and the reductive methylation of said imino ether are sequentially carried out with a noble metal catalyst and hydrogen in the presence of formaldehyde, or a source thereof, wherein both reactions can be conducted in the same reaction vessel.

Abstract: 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.

Abstract: 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.

Abstract: 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:Rh Cl.sub.3 [N{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.3 ].sub.10Rh Cl.sub.3 [N{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.3 ].sub.12Rh Cl.sub.3 [N{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.3 ].sub.15Rh Cl.sub.3 [HN{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.2 ].sub.4Rh Cl.sub.3 [HN{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.2 ].sub.8permitting easy recovery of the rhodium, by simple filtration.