摘要:
The present invention relates to a process for the preparation of {2-[4-(α-phenyl-p-chlorobenzyl)-piperazin-1-yl]-ethoxy}-acetic acid-N,N-dimethylamide of the Formula (I) and enantiomers thereof. The compound of the Formula (I) or enantiomers thereof are important pharmaceutical intermediates suitable for direct transformation into non-sedating antihistamine type pharmaceutical active ingredients cetirizine and levocetirizine.
摘要:
According to the present invention, 2-chloroethoxy-acetic acid-N,N-dimethylamide of the Formula (I) is prepared by reacting 2-hydroxyethoxy-acetic acid-N,N-dimethylamide of the Formula (II) in a solvent optionally in the presence of a catalyst with thionyl chloride and removing the solvent by distillation.
摘要:
The present invention is related to 1-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.
摘要:
The invention refers to a novel process for the preparation of {2-[-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy}acetic acid, which comprises hydrolyzing an N,N-disubstituted {2-[-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy}acetamide, wherein said substituents are selected from alkyl groups having 1 to 4 carbon atoms optionally substituted by a phenyl group, alkenyl groups having 2 to 4 carbon atoms or cyclohexyl groups, or the substituents together with the adjacent nitrogen atom of the acetoamido group, form a morpholino group.
摘要:
The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.
摘要:
The present invention relates to a new method of preparation of the polymorph form 1 of methyl (S)-(+)-(2-chlorophenyl)-2-(6,7-dihydro4H-thieno[3,2-c]pyridine-5-yl-acetate hydrogensulfate of the formula (I).
摘要:
The invention relates to a process for the preparation of amorphous atorvastatin calcium by recrystallization of crude atorvastatin from an organic solvent which comprises dissolving crude amorphous atorvastatin calcium in a lower alkanol containing 2-4 carbon atoms or a mixture of such alkanols under heating and isolating the amorphous atorvastatin calcium precipitated after cooling. The atorvastatin calcium obtained is a known valuable agent useful in treating hyperlipidemia and hypercholestrolemia.
摘要:
The invention relates to a process for the preparation of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno-[2,3-b][1,5]benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno [2,3-b][1/5]benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1,3-dimethyl-2-imidazolidinone. The invention also encompasses new 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno [2,3-b][1,5]benzodiazepine dihydrochloride trihydrate of the formula (IB), the preparation thereof and pharmaceutical compositions comprising said new compound.
摘要:
The present invention relates to the use of novel vildagliptin complexes for the manufacture of high purity vildagliptin of Formula I and/or pharmaceutical acceptable salts thereof. Further objects of the present invention are pharmaceutically acceptable complexes of vildagliptin and/or amorphous and crystalline forms, anhydrous forms, amorphous and crystalline hydrates, amorphous and crystalline solvates of the complexes and a process for the preparation thereof. Another object of the present invention is the high purity vildagliptin and pharmaceutically acceptable salts thereof prepared form the vildagliptin complexes of the present invention, a process for the preparation thereof and pharmaceutical compositions containing vildagliptin base, pharmaceutically acceptable salts and/or complexes and use thereof for the treatment of type 2 diabetes (NIDDM). The present invention provides pharmaceutically advantageous high purity vildagliptin complexes.
摘要:
The present invention relates to a new process for the preparation of rosuvastatin [7-[4-(4-Fluorophenyl)-6-isopropyl-2-(methanesulphonyl-methyl-amino)-pyrimidin-5-yl]-(3R,51S)-dihydroxy-hept-6-enoic acid] of the formula (I) salts formed with bivalent cations, preferably with calcium or zinc ions, characterized in that rosuvastatin tert.-butylammonium salt is reacted with the appropriate bivalent cation, preferably with calcium or zinc ions in a mixture of a water immiscible or slightly miscible organic solvent and water and the formed salt is isolated.