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: The present invention is directed to novel processes for the preparation of paricalcitol to novel intermediates used in these processes, and to processes for preparation of the novel intermediates.

Abstract: The present invention is directed to novel processes for the preparation of paricalcitol to novel intermediates used in these processes, and to processes for preparation of the novel intermediates.

Abstract: The present invention provides a novel polymorphic form of olopatadine hydrochloride ([(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride), a selective histamine H1-receptor antagonist that is used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. The present invention also provides novel methods for producing olopatadine on a large scale, and in a manner that is cost effective, provides a low level of impurities and eliminates the need to use the costly and dangerous base, butyllithium, which is used in prior art reactions for making olopatadine. The present invention further provides novel processes for carrying out a large scale production of 3-dimethylaminopropyltriphenylphosphonium bromide and its corresponding hydrobromide salt, which are employed in the production of olopatadine, and pharmaceutically acceptable salts of olopatadine.

Abstract: A process of making racemic [2S*[R*[R*[R*]]]] and [2R*[S*[S*[S*]]]]-(±)?,??-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] of the compound of the formula (I) and its pure [2S*[R*[R*[R*]]]]- and [2R*[S*[S*[S*]]]]-enantiomer compounds and pharmaceutically acceptable salts thereof.

Abstract: A process of making racemic [2S*[R*[R*[R*]]]] and [2R*[S*[S*[S*]]]]-(±)?,??-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] of the compound of the formula (I) and its pure [2S*[R*[R*[R*]]]]- and [2R*[S*[S*[S*]]]]-enantiomer compounds and pharmaceutically acceptable salts thereof.

Abstract: The invention concerns a method for preparing optionally substituted 3-indolcarboxylic acid esters, with hexahydro-8-hydroxy-2,6-methano-2H-chinolizin-3(4H)-one. The invention is characterized in that the optionally substituted 3-indolcarboxylic acid is converted by means of a suitable halogenating agent, into corresponding acid halide, preferably corresponding acid chloride, and the latter is transformed with hexahydro-8-hydroxy-2,6-methano-2H-chinolizin-3(4H)-one. The invention is characterized in that the entire reaction occurs in acid medium with a maximum pH of 7.

Abstract: The present invention provides a novel polymorphic form of olopatadine hydrochloride ([(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride), a selective histamine H1-receptor antagonist that is used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. The present invention also provides novel methods for producing olopatadine on a large scale, and in a manner that is cost effective, provides a low level of impurities and eliminates the need to use the costly and dangerous base, butyllithium, which is used in prior art reactions for making olopatadine. The present invention further provides novel processes for carrying out a large scale production of 3-dimethylaminopropyltriphenylphosphonium bromide and its corresponding hydrobromide salt, which are employed in the production of olopatadine, and pharmaceutically acceptable salts of olopatadine.

Abstract: A process of making racemic [2S*[R*[R*[R*]]]] and [2R*[S*[S*[S*]]]]-(±)?,??-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] of the compound of the formula (I) and its pure [2S*[R*[R*[R*]]]]- and [2R*[S*[S*[S*]]]]-enantiomer compounds and pharmaceutically acceptable salts thereof.

Abstract: A method for preparing optionally substituted {N-[1-(S)-carbalkoxy-3-phenylpropyl]-S-alanyl-2S,3aR,7aS-octahydroindole-2-carboxylic acid} and pharmaceutically acceptable salts thereof, wherein a racemic mixture of optionally substituted trans-octahydroindole-2-carboxylic acid is reacted with the N-carboxyanhydride of {N-[1-(S)-alkoxycarbonyl-3-phenylpropyl]-L-alanine}, which is optionally substituted on the phenyl ring, in a suitable inert solvent, and subsequently the resulting optionally substituted {N-[1-S-carbalkoxy-3-phenylpropyl]-S-alanyl-2S,3aR,7aS-octahydroindole-2-carboxylic acid}, preferably trandolapril, is isolated, and polymorphic forms A and B of trandolapril.

Abstract: The invention relates to a process for preparing substituted cyclopentane derivatives represented by the formula (I) wherein R1, R2, R3, R4, X and Y are as described in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to a process for purifying the compound of formula (Ia) and novel crystalline forms of the compound of formula (Ia).

Abstract: The invention relates to a process for preparing substituted cyclopentane derivatives represented by the 1