Abstract: The present invention provides processes for producing isoquinolinium compounds, and for converting them into cisatracurium salts, e.g.

Abstract: The present invention provides an improved method for obtaining cisatracurium besylate, which preferably chromatographically separating cisatracurium besylate from a mixture of (1R,1?R)-atracurium isomers via flash chromatography

Abstract: Provided are novel salts of 2-(1-azabicyclo-[2.2.

Abstract: The present invention provides novel isoquinolinium compounds, methods of producing the isoquinolinium compounds, and methods for converting them into cisatracurium, e.g., cisatracurium besylate.

Abstract: Derivatives of 1,2-benzisoxazole-3-methanesulfonic acid, which are non-hygroscopic and non-hydrated and their use as intermediates from the preparation of zonisamide are disclosed. Further disclosed are processes of preparing zonisamide from these 1,2-benzisoxazole-3-methanesulfonic acid derivatives, processes of preparing exemplary 1,2-benzisoxazole-3-methanesulfonic acid derivatives and crystalline forms of exemplary 2-benzisoxazole-3-methanesulfonic acid derivatives. A novel process of preparing zonisamide is also disclosed.

Abstract: The present invention provides an improved method of chromatographically separating the isomers of (1R,rR)-atracurium salts by high-performance liquid chromatography (HPLC), in the absence of a strong acid. The separation is preferably performed on a silica gel HPLC column using an eluent containing an organic solvent, a polar aprotic co-solvent and a weak organic acid.

Abstract: Provided is a method for separating cisatracurium from a mixture of atracurium isomers, which method includes eluting from a Reverse Phase (RP) stationary phase with a mobile phase in which the isomers are stable. The method of the present invention can be conveniently and inexpensively scaled up.

Abstract: The present invention provides a process for preparing highly pure 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (imiquimod). The process preferably includes heating 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (II) with ammonia in a polar aprotic solvent at relatively moderate pressure to produce imiquimod, and optionally purifying the imiquimod. The process of the present invention can produce highly pure imiquimod in high yield.

Abstract: Disclosed are novel crystalline forms of Temozolomide, methods of preparation thereof, medicaments including the novel crystalline forms of Temozolomide, and uses thereof in the treatment of medical conditions.

Abstract: Disclosed are novel crystalline forms of Temozolomide, methods of preparation thereof, medicaments including the novel crystalline forms of Temozolomide, and uses thereof in the treatment of medical conditions.

Abstract: The present invention provides a process for preparing highly pure Temozolomide base which includes recovery from the purification mother liquors by using an anionic exchange resin. By treating Temozolomide hydrochloride with a mixture of an organic acid, a water miscible organic solvent, and water, Temozolomide free base is obtained in an acidic medium. Due to the high sensitivity of Temozolomide to basic pH values the recovery-including process is especially advantageous because it enables obtaining high yields of highly pure Temozolomide base in acidic conditions. The process for producing Temozolomide base includes hydrolysis of the starting material 8-cyano-3-methyl-[3H]-imidazo[5,1-d]-tetrazin-4-one in acidic medium to obtain highly pure Temozolomide hydrochloride in high yield.

Abstract: The present invention provides a crystalline donepezil maleate, which is used as an intermediate in the preparation of donepezil hydrochloride. Also provided are novel processes for producing same in substantially pure form and a process for producing pharmaceutically pure amorphous donepezil hydrochloride therefrom.

Abstract: The present invention provides processes for preparing intermediates useful in the preparation of gemcitabine and other nucleosides, and processes for preparing gemcitabine therewith. Exemplary intermediates include mixtures of D-erythro and D-threo isomers of 3-(hydroxy)-2,2-difluoro-3-(2,2-dimethyldioxolan-4-yl)-propionic acid salts. Also provided is a process for selectively isolating the D-erythro and D-threo isomers of D-erythro and D-threo isomers of 3-(hydroxy)-2,2-difluoro-3-(2,2-dimethyldioxolan-4-yl)-propionic acid salts, and processes for using such isomers in the preparation of nucleoside analogs such as, e.g., gemcitabine, intermediates thereof, and analogs thereof.

Abstract: A novel process for preparing (2?,3?,5?,16?,17?)-17-acetoxy-3-hydroxy-2-(4-morpholinyl)-16-(1-pyrrolidinyl) androstane, a known intermediate in the synthesis of the skeletal muscle relaxant rocuronium bromide, is disclosed.

Abstract: The present invention provides a novel montelukast intermediate and a simple and straightforward process for preparing it. According to the present invention, by using this intermediate and the process, essentially as described herein, montelukast acid and salts thereof are obtained.

Abstract: Provided is a process for producing imatinib and salts thereof, e.g., imatinib mesylate. The process includes reacting 4-(4-methyl-piperazin-1-ylmethyl)-benzoic acid with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidine-amine in the presence of a carboxylic acid coupling reagent, to produce imatinib, and optionally converting the imatinib into a salt.

Abstract: An amorphous form of montelukast sodium and a montelukast sodium lactose co-precipitate, processes for producing same, pharmaceutical compositions containing same and methods of treatment utilizing same are disclosed.

Abstract: Provided is a method for preparing letrozole, which includes reacting an activated bis-(4-cyanophenyl)-methane with a triazole to produce letrozole, and, optionally, purifying the letrozole. Also provided are highly pure letrozole, and a method of purifying letrozole, which method includes precipitating letrozole, e.g., by selective precipitation from a reaction mixture and/or by subjecting the letrozole to one or more crystallizations.

Abstract: The present invention provides a process for preparing highly pure montelukast and salts thereof by reacting the side-chain precursor 1-(mercaptomethyl)-cyclopropaneacetic acid with 2-(2-(3S)-(3-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(methanesulfonyloxypropyl)phenyl-2-propanol in a solvent mixture containing a base.

Abstract: A novel process for preparing highly pure cilostazol, effected by reacting 6-hydroxy-3,4-dihydroquinolinone and 5-(4-chlorobutyl)-1-cyclohexyl-1H-tetrazole in the presence of a hydrated inorganic base, is disclosed. Further disclosed is highly pure cilostazol, and particularly highly pure cilostazol that is substantially free of 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-butoxy]-1-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-butyl ]-3,4-dihydro-1H-quinolin-2-one.