Abstract: Present invention represents process for the preparation of HMG-CoA reductase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain.

Abstract: The present invention relates to a cabergoline crystal form L, its preparation from halogenated aromatic solvents and aliphatic hydrocarbons and to pharmaceutical compositions containing the new form.

Abstract: Genetically modified strains of Streptomyces tsukubaensis (S. tsukubaensis) can be used for an improved fermentation process for the preparation of tacrolimus or a salt or derivative thereof by cultivation of these genetically modified strains. Novel genes allowing biosynthesis of allylmalonyl-CoA can be used for polyketide production with allylmalonyl extender unit.

Abstract: Process for the preparation of enantiomerically pure methyl ester of rosuvastatin has been developed, wherein the crude methyl ester ester is first purified by preparative chromatography, followed by crystallization.

Abstract: A novel synthesis of statins uses Wittig reaction of a heterocyclic core of statin with a lactonized side chain already possessing needed stereochemistry. Any separation of diastereoisomers is performed early in the course of synthesis.

Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of ?-amino boronic acid derivatives.

Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of halogenoalkanes.

Abstract: The present invention relates to a process for removing an organic solvent from a salt of omeprazole, in particular a magnesium salt of omeprazole, a composition comprising a salt of omeprazole, in particular a magnesium salt of omeprazole obtainable by such a process, and pharmaceutical compositions comprising said composition or a salt of omeprazole, in particular a magnesium salt of omeprazole, in particular where omeprazole is S-omeprazole.

Abstract: The present invention belongs to the field of pharmaceutical industry and relates to novel crystalline omeprazole sodium ethanol solvate and to the process for its preparation, which acts as intermediary compound to the processes for its conversion into different crystalline forms, first of all to a known omeprazole sodium form A, with low amount of residual solvents, i.e. less than 0.5% by weight of residual solvent. The present invention also relates to novel crystalline omeprazole sodium form E and crystalline omeprazole sodium form F as well to the processes for their preparation as well, both with considerably low levels of residual solvents. Omeprazole sodium form A and both novel crystalline forms omeprazole sodium form E and form F are useful for the treatment of gastrointestinal disorders.

Abstract: The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.

Abstract: A process for the manufacturing of a pure irbesartan comprising converting irbesartan or a protected derivative thereof into an isolated hydrohalide acid addition salt, whereupon said hydrohalide acid addition salt is converted into the irbesartan is described.

Abstract: A new process for preparing pure amorphous rosuvastatin calcium, substantially free of impurities, is disclosed. A process comprising hydrolysing a C1 to C5 alkyl ester of rosuvastatin, preferably methyl rosuvastatin or tert-butyl rosuvastatin, with a base, e.g. sodium hydroxide, in the presence of an aprotic solvent, preferably tetrahydrofuran and N,N-dimethyl acetamide, or in the presence of a mixture of an aprotic solvent and water, to obtain a solution of rosuvastatin salt, which may be converted to another rosuvastatin salt using another cation, e.g. with calcium cation to obtain rosuvastatin calcium. Rosuvastatin amine salts may be obtained as well. In another preferred aspect of the invention rosuvastatin free acid may be converted to various rosuvastatin salts, e.g. to rosuvastatin calcium, rosuvastatin sodium or various rosuvastatin amine salts, including rosuvastatin solvates, e.g. rosuvastatin calcium hydrate.

Abstract: The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses a process for preparing 3-amino-2,2-dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processes for preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents.

Abstract: A new process for preparation of 3-(2-hydroxy-5-substituted phenyl)-N,alkyl-3-phenylpropylamines from cinnamyl chloride via N-alkyl-3-phenylprop-2-en-1-amine has been developed.

Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing dosage forms containing ezetimibe, comprising the steps of: a) providing a composition comprising ezetimibe, b) sieving a composition comprising a composition of step (a), c) shear mixing of the composition after step (b), preferably the mixing of the composition is carried out by high shear mixing, d) formulation into a dosage form. The present invention also relates to dosage forms containing ezetimibe and ezetimibe and simvastatin, which have been prepared according to the process according to the invention.

Abstract: The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.

Abstract: The present invention provides a pharmaceutical composition comprising at least one active pharmaceutical ingredient comprising sulphonylurea moiety, wherein the at least one active pharmaceutical ingredient comprising sulphonylurea moiety is intimately mixed with a basic agent. The weight ratio of the basic agent and the at least one active pharmaceutical ingredient comprising sulphonylurea moiety is from 2.5:1 to 50:1, preferably from 2.5:1 to 25:1, more preferably from 3.5:1 to 15:1, yet more preferably from 3.5:1 to 10:1. The pharmaceutical composition can be obtained by simply mixing active pharmaceutical ingredient comprising sulphonylurea moiety and the basic agent in the aforementioned weight ratio, optionally in the presence of the granulation liquid. Alternatively, the pharmaceutical composition can be obtained by at least partially or fully dissolving the compounds in the granulation liquid or solvent, and at least partly precipitating them.

Abstract: The present invention belongs to the field of pharmaceutical industry and relates to dosage forms comprising active pharmaceutical ingredients (API) such as tadalafil, simvastatin, fenofibrate and lovastatin that are practically insoluble in water, adsorbed on a carrier. Furthermore it relates to an adsorbate comprising API being practically insoluble in water and to a process for the preparation of said adsorbate with non-polar solvent (s) such as chlorinated hydrocarbon, diisopropylethes and hexane. Furthermore the invention relates to a process for the preparation of the dosage form, as well as to the use of the adsorbate for the preparation of the dosage form. Moreover it relates to the dosage form for use in the treatment of erectile dysfunction, human immunodeficiency virus (HIV) infections and/or Acquired Immune Deficiency Syndrome (AIDS).

Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of 1-(2,3-dihydrobenzofuran-4-yl)ethanone, an intermediate in preparation of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide, i.e. ramelteon.

Abstract: The present invention relates to novel pharmaceutically acceptable salts of sitagliptin, to processes for their preparation and to pharmaceutical compositions containing them.