Abstract: A dust-reduced nicotine-containing granulate comprising a homogenous mixture of nicotine or a pharmaceutically acceptable nicotine derivative and an excipient, the granulate having a particle size of at least 150 ?m. Method for the preparation of a dust-reduced nicotine-containing granulate, and use of the nicotine-containing granulate for the preparation of pharmaceutical products.

Abstract: The present invention relates to the preparation of ?-substituted ?-amino carboxylic acids, preferably in enantiomerically enriched or even enantiomerically pure form, by a one-pot conversion of a ?-substituted ?-nitro dicarboxylic acid ester or of a ?-substituted ?-nitro dicarboxylate of general formula to a ?-substituted ?-nitro carboxylic acid and a subsequent reduction of the ?-nitro group to an amine group. In particular, the present invention relates to the preparation of (S)-pregabalin. In addition, the formation of enantiomerically enriched ?-substituted ?-amino carboxylic acids and ?-substituted ?-nitronate carboxylic acid salts are also described.

Abstract: The present invention relates to the preparation of ?-substituted ?-amino carboxylic acids, preferably in enantiomerically enriched or even enantiomerically pure form, by a one-pot conversion of a ?-substituted ?-nitro dicarboxylic acid ester or of a ?-substituted ?-nitro dicarboxylate of general formula to a ?-substituted ?-nitro carboxylic acid and a subsequent reduction of the ?-nitro group to an amine group. In particular, the present invention relates to the preparation of (S)-pregabalin. In addition, the formation of enantiomerically enriched ?-substituted ?-amino carboxylic acids and ?-substituted ?-nitronate carboxylic acid salts are also described.

Abstract: A nicotine-containing product comprising a pharmaceutically acceptable polymeric substrate, which is able to bind cations, nicotine or a pharmaceutically acceptable nicotine derivative, and pharmaceutically acceptable inorganic cations. It further pertains to a method for the preparation of such a nicotine-containing product and to the use thereof for the preparation of a pharmaceutical product.

Abstract: A kit including a packaging material and a solid pharmaceutical or nutraceutical product, and in particular for a solid, opioid-based pharmaceutical product. The packaging material has an inner surface and an outer surface that avoids contamination of the product. At least that part of the inner surface, which is exposed to the pharmaceutical or nutraceutical product, is made of or covered with an inert material selected from the group made of polyamide, polyethylene terephthalate and epoxy resin-coated aluminium.

Abstract: A kit including a packaging material and a solid pharmaceutical or nutraceutical product, and in particular for a solid, opioid-based pharmaceutical product. The packaging material has an inner surface and an outer surface that avoids contamination of the product. At least that part of the inner surface, which is exposed to the pharmaceutical or nutraceutical product, is made of or covered with an inert material selected from the group made of polyamide, polyethylene terephthalate and epoxy resin-coated aluminium.

Abstract: The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is achieved by reacting a starting compound with a compound of general formula R1OOC—N?N—COOR2 in a suitable solvent.

Abstract: The present invention relates to a process for the preparation of quaternary N-alkyl morphin or morphinan alkaloid derivatives. This is achieved by using a nucleophilic nitrogen, phosphor or sulfur containing base in the reaction mixture.

Abstract: A nicotine-containing product comprising a pharmaceutically acceptable polymeric substrate, which is able to bind cations, nicotine or a pharmaceutically acceptable nicotine derivative, and pharmaceutically acceptable inorganic cations. It further pertains to a method for the preparation of such a nicotine-containing product and to the use thereof for the preparation of a pharmaceutical product.

Abstract: A dust-reduced nicotine-containing granulate comprising a homogenous mixture of nicotine or a pharmaceutically acceptable nicotine derivative and an excipient, the granulate having a particle size of at least 150 ?m. Method for the preparation of a dust-reduced nicotine-containing granulate, and use of the nicotine-containing granulate for the preparation of pharmaceutical products.

Abstract: A process for preparing 17?-substituted 4-azaandrost-1-en-3-one compounds of the general formula (I): or a pharmaceutically approved salt thereof, where R is hydroxyl, optionally substituted, linear or branched (C1-C2)alkyl or (C1-C12)alkenyl; phenyl or benzyl; an —OR1 radical, or an —NHR1 radical, or an —NR1R2 radical; R1 is hydrogen, optionally substituted, linear or branched (C1-C12)alkyl or (C1-C12)alkenyl, or optionally substituted phenyl; R2 is hydrogen, methyl, ethyl or propyl; or —NR1R2 is a 5- or 6-membered heterocyclic ring, by (A) introducing protecting groups into the 3-keto-4-aza moiety of the corresponding 1,2-dihydro compound, so that a compound of the general formula (III) is formed: where R3 is trialkylsilyl or, together with R4, the —C(O)—C(O)— or —C(O)—Y—C(O)— radical; R4 is alkyloxycarbonyl or phenyloxycarbonyl, preferably Boc (=tert-butyloxycarbonyl); or trialkylsilyl, or, together with R3, the —C(O)—C(O)— or —C(O)—Y—C(O)— radical; Y is —[C(R5)(R6)]n— or —CH(R5)?CH(R6)—, or ort

Abstract: The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is achieved by reacting a starting compound with a compound of general formula R1OOC—N?N—COOR2 in a suitable solvent.

Abstract: The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is achieved by reacting a starting compound with a compound of general formula R1OOC—N?N—COOR2 in a suitable solvent.

Abstract: The present invention relates to a method for the preparation of a carboxylic imide having the general formula R1—(CO)—(NR3)—(CO)—R2??(I), wherein a carboxylic anhydride having the general formula R1—(CO)—O—(CO)—R2??(II) is reacted with urea or a urea derivative of the form (R3HN)—(CO)—(NR3H) in a solvent. In particular, the method can be used for the preparation of thalidomide.

Abstract: The present invention relates to a method for the preparation of a carboxylic imide having the general formula R1—(CO)—(NR3)—(CO)—R2 , ??(I) wherein a carboxylic anhydride having the general formula R1—(CO)—O—(CO)—R2 ??(II) is reacted with urea or a urea derivative of the form (R3HN)—(CO)—(NR3H) in a solvent. In particular, the method can be used for the preparation of thalidomide.

Abstract: Disclosed is a method for producing d-threo-[R(R*,R*)]-2-phenyl-2-piperidine-2-yl acetate and the acid addition salts thereof by converting d-threo-[R(R*,R*)]-2-phenyl-2-piperidine-2-yl ethanoic acid or an acid addition salt thereof into the corresponding d-threo-[R(R*,R*)]-2-phenyl-2-piperidine-2-yl ethanoic acid halide, producing the desired d-threo-[R(R*,R*)]-2-phenyl-2-piperidine-2-yl-acetate or an acid addition salt thereof by means of esterification, and optionally recrystallizing the obtained product. The invention also relates to methods for producing pure threo-2-phenyl-2-piperidine-2-yl acetamide or the starting material for producing d-threo-[R(R*,R*)]-2-phenyl-2-piperidine-2-yl ethanoic acid.