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 herein a two-step process for preparing pharmaceutically pure quetiapine and salts thereof by obtaining the starting material 11-chloro-dibenzo-thiazepine followed by reacting the 11-chloro-dibenzo-thiazepine with 1-(2-hydroxyethoxy)ethylpiperazine, or its salt, in the presence of an inorganic or organic base in an organic solvent or in a two-phase solvent system. The present invention provides also a novel, one-pot reaction process for preparing pharmaceutically pure quetiapine and salts thereof. The two processes provided herein can be easily, conveniently and inexpensively scaled-up.

Abstract: Processes are provided herein for the preparation of pure rocuronium bromide and for the purification of impure rocuronium bromide obviating the need for column chromatography and that can be easily, conveniently and inexpensively scaled-up.

Abstract: Processes are provided herein for the preparation and purification of stable, powdered solids comprising substantially pure rocuronium bromide.

Abstract: The present invention provides novel processes for purifying anastrozole, devoid of using liquid chromatography. The purification processes are via the isolated anastrozole salt forms, either by crystallization or by selective acidic extractions, and optionally in both cases, converting the purified anastrozole salt to anastrozole base. Also provided is an improved process for the synthesis of anastrozole, which is obtained by alkylating the isolated and purified starting material 3,5-bis(2-cyanoprop-2-yl)benzylbromide, the process being devoid of using toxic, hazardous and environmental unfriendly solvents and reagents.

Abstract: Derivatives of 1,2-benzisoxazole-3-methanesulfonic acid, which are non-hygroscopic and non-hydrated and their use as intermediates fro 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: Provided is a method for reprocessing neuromuscular blocking agents containing a quaternary ammonium salt, e.g., Rocuronium bromide, using a novel dealkylation method. The process is effective in obtaining a highly pure product from a contaminated starting material by heating, optionally in the presence of an organic solvent, to produce a dealkyated product. The dealkylated product is purified, e.g., by crystallization, and converted by any known method to a stable, highly-pure neuromuscular blocking agent.

Abstract: Disclosed is a process of preparing 1,2-benzisoxazole-3-methanesulfonamide (zonisamide). Also disclosed is a method of dehydrating sodium 1,2-benzisoxazole-3-methanesulfonate, a compound useful in the preparation of 1,2-bisoxazole-3-methanesulfonamide (zonisamide) as well as new crystalline forms of sodium 1,2-benzisoxazole-3-methanesulfonate.

Abstract: An improved process for preparing fluticasone propionate, performed in the presence of water, is disclosed. Further disclosed is a process for preparing a fluticasone propionate that is highly suitable for administration by inhalation. Further disclosed are fluticasone propionate and a powdered fluticasone propionate prepared by these processes and pharmaceutical compositions for administration by inhalation containing same. A process of purifying a key intermediate in the synthesis of fluticasone propionate is also disclosed.

Abstract: A process for the preparation of Terbinafine and salts thereof by reacting 1-chloro-6,6-dimethylhept-2-en-4-yne and N-methyl-N-(1-naphthylmethyl)amine in a basic aqueous medium is disclosed. Also disclosed is a process for the preparation of 1-chloro-6,6-dimethylhept-2-en-4-yne.

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.

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: The invention provides stable amorphous calcium pseudomonate.

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 invention provides a stable and easy to formulate amorphous solid, suitable for the preparation of solid pharmaceutical compositions comprising a mixture of an amorphous active pharmaceutical ingredient and at least one pharmaceutically acceptable inactive ingredient.

Abstract: The invention provides a process for the preparation of a compound of the formula 6 comprising the hydrolysis and decarboxylation of a compound of the formula 5 according to the reaction: wherein R and R2 independently a C1-C4 alkyl group or an aralkyl group.

Abstract: The invention provides a process for preparing 1-methylindazole-3-carboxylic acid of formula (I): 1

Abstract: The present invention provides a crystalline halobetasol propionate selected from the group consisting of halobetasol propionate having crystalline Form I characterized by power X-ray diffraction peak positions and intensities as set forth in Table 1 herein, halobetasol propionate having crystalline Form II characterized by power X-ray diffraction peak positions and intensities as set forth in Table 2 herein, halobetasol propionate having crystalline Form III characterized by power X-ray diffraction peak positions and intensities as set forth in Table 3 herein, halobetasol propionate having crystalline Form IV characterized by power X-ray diffraction peak positions and intensities as set forth in Table 4 herein, halobetasol propionate having crystalline Form V characterized by power X-ray diffraction peak positions and intensities as set forth in Table 5 herein, and halobetasol propionate having crystalline Form VI characterized by power X-ray diffraction peak positions and intensities as set forth in Table 6

Abstract: The present invention provides a crystalline halobetasol propionate selected from the group consisting of halobetasol propionate having crystalline Form I characterized by power X-ray diffraction peak positions and intensities as set forth in Table 1 herein, halobetasol propionate having crystalline Form II characterized by power X-ray diffraction peak positions and intensities as set forth in Table 2 herein, halobetasol propionate having crystalline Form III characterized by power X-ray diffraction peak positions and intensities as set forth in Table 3 herein, halobetasol propionate having crystalline Form IV characterized by power X-ray diffraction peak positions and intensities as set forth in Table 4 herein, halobetasol propionate having crystalline Form V characterized by power X-ray diffraction peak positions and intensities as set forth in Table 5 herein, and halobetasol propionate having crystalline Form VI characterized by power X-ray diffraction peak positions and intensities as set forth in Table 6

Abstract: The invention provides a process for the preparation and isolation of compound of formula 2, comprising the following steps: oxidizing Flumethasone dissolved in a tetrahydrofuran-water mixture with periodic acid at a temperature lower than 30° C.; cooling the reaction mixture to a temperature lower than 10° C.; adding an antisolvent precooled to a temperature lower than 10° C.; and separating the precipitated crystal by filtration, whereby there is obtained a compound of formula 2 in a yield of at least 98% and of a chromatographic purity of at least 99%.