Abstract: A process for preparing substituted pyrrolidine compounds, including (5)-2-{1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphenylacetamide hydrobromide, commonly known in the art as darifenacin, comprising reacting a pyrrolidine compound with a benzofuran derivative in the presence of a phase-transfer catalyst.

Abstract: The invention relates to a process for tightly controlling the particle size of cinacalcet hydrochloride, i.e. a process for preparing large or small crystals of cinacalcet hydrochloride, which yields cinacalcet hydrochloride in a narrow, reproducible and consistent distribution of particles, which hence does not require to reprocess, rework or destroy material of undesired size, which is efficient and cost-effective, and which is suitable for industrial implementation.

Abstract: The invention relates to polymorphic crystalline forms of aripiprazole, synthetic processes for their preparation and pharmaceutical compositions containing the same. These crystalline forms of aripiprazole can be readily milled and can be easily combined with various pharmaceutical adjuvants without effecting changes to their crystalline structure when, for example, pressed into tablet or capsule form.

Abstract: The invention relates to an improved process for the preparation of duloxetine hydrochloride.

Abstract: The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][1,4]thiazepin-11(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo[bf][1,4]thiazepine. Thereafter, the 11-chloro-dibenzo[bf][1,4]thiazepine is reacted with 2-(2-piperazin-1-ylethoxy)-ethanol to yield, following several processing steps, quetiapine. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations.

Abstract: The invention relates to the preparation of losartan and losartan potassium. More particularly, the invention relates to the preparation of losartan and losartan potassium in a simplified process that provides higher purity losartan potassium and losartan potassium having larger crystal sizes. The invention further includes formulating into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans.

Abstract: The present invention relates to an improved process for preparation of Voriconazole and Voriconazole (1R)-(?)-10-camphorsulfonate.

Abstract: The present invention relates to amorphous form darifenacin hydrobromide and processes therefor. In addition, the present invention relates to compositions comprising amorphous form darifenacin hydrobromide.

Abstract: The present invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity, of darifenacin and its intermediate compounds and salts thereof. In addition, the invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity of compounds of formula (I): wherein Y is hydrogen or a substituent of the formula: including the differentiation and quantification of compounds of formula (I) of varying enantiomeric purity from their corresponding enantiomers. The invention further relates to a process for preparing enantiomerically pure darifenacin using enantiomerically pure starting compounds which have been previously differentiated and quantified according to the method of the invention.

Abstract: The present invention relates to a process for preparing racemic narwedine (which can be can be kinetically resolved) to yield (?)-narwedine and which is the biogenic precursor of (?)-galanthamine) and the use thereof as a starting material for producing (?)-galanthamine. The invention further includes processes for preparing (?)-galanthamine and (?)-galanthamine hydrobromide, as well as related novel compounds.

Abstract: The invention includes an improved process for producing tamsulosin comprising reacting 5-(2-aminopropyl)-2-methoxybenzenesulfonamide with 2-(o-ethoxyphenoxy)ethyl bromide in an organic phosphite solvent to obtain tamsulosin. Optically pure (R)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide can be employed to produce optically pure (R)-tamsulosin product. The organic phosphite solvent utilized in the reaction can include tri-alkyl phosphites such as triethyl phosphite, trimethyl phosphite, and tributyl phosphite. Additionally, processes for producing tamsulosin having a low concentration of by-product contaminants, such as 5-((R)-2-{Bis-[2-(2-ethoxyphenoxy)ethyl]amino}-propyl)-2-methoxybenzenesulfonamide, and the use of such by-products to monitor the chemical purity of tamsulosin, are provided.

Abstract: The invention relates, in general, to a new solid crystalline form of pantoprazole free acid (denominated “Form III”), salts derived therefrom (e.g., pantoprazole sodium and pantoprazole sodium sesquihydrate) and methods for producing the same. The invention further includes formulating pantoprazole free acid Form III, salts derived therefrom (e.g., pantoprazole sodium and pantoprazole sodium sesquihydrate) and/or in vivo cleavable prodrugs thereof (collectively “the compounds of the invention”) into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans.

Abstract: The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to a novel process for the preparation of montelukast sodium, a compound of Formula (1b) and precursors thereof. The invention further concerns the free acid of this compound in crystalline form, obtainable for the first time by the new process.

Abstract: Improved process for manufacturing mirtazapine. A process is described for preparing mirtazapine starting from a compound of formula (II), which is subjected to a ring cyclization, obtaining mirtazapine for pharmaceutical use in crystalline and anhydrous form.

Abstract: The present invention relates to a process for preparing vildagliptin of formula (I) with high chemical and enantiomeric purity and compositions comprising vildagliptin. In addition, the present invention relates to (2S,2?S)-1,1?-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)imino]bis(1-oxo-2,1-ethanediyl)]di(2-pyrrolidinecarbonitrile) of formula (II), processes for preparing, and compositions comprising a compound for formula (II). Furthermore, the invention relates to processes for determining the purity of vildagliptin using a compound of formula (II).

Abstract: The present invention relates to a novel compound of formula (IV) which is an intermediate that can be used for the preparation of pioglitazone. It also relates to a method of obtaining the novel compound (IV) starting from the natural product L-tyrosine, in which the amino group is protected in the form of aromatic imino group, and a method of obtaining pioglitazone from the said intermediate.

Abstract: The present invention relates to a process for the preparation of 5-{4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl-2,4-thiazolidinedione of formula (I) (Rosiglitazone), which comprises the reaction of 5-{4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzylidene-2,4-thiazolidinedione of formula (II), with a 1,4-dihydropyridine of general formula (III).

Abstract: The present invention relates to a process for the preparation of 5-{4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl-2,4-thiazolidinedione of formula (I) Rosiglitazone), which comprises the reaction of 5-{4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxyl]benzylidene-2,4-thiazolidinedione of formula (II), with a 1,4-dihydropyridine of general formula (III).

Abstract: The present invention is directed to intermediate compounds of mirtazapine and methods for obtaining same. A method is described for obtaining (±)-3-phenyl-1-methylpiperazine, an important intermediate for obtaining mirtazapine, which is based on imposing a cyclization reaction, in the presence of a reducing agent, on new compounds of general formula (1) in which Z is a leaving group capable of undergoing a nucleophilic displacement. A method is also described for obtaining the new compounds of formula (1).