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. The isoquinolinium compounds of the present invention can be obtained in the form of solids, which can be purified using simple techniques and can be used to afford pure cisatracurium besylate without HPLC purification.

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

Abstract: The present invention provides compounds which are useful, e.g., as reference markers for analyzing the purity of cisatracurium and salts thereof, a test method for determining the said purity and processes for preparing reference markers.

Abstract: Provided is a process for producing highly pure 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (imiquimod), which includes reacting 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline with a non-gaseous amine precursor. Also provided are methods for isolating highly pure imiquimod. Further provided are intermediates useful in the production of imiquimod, methods for producing such intermediates, and methods for obtaining imiquimod from such intermediates.

Abstract: The present invention provides a process of producing cisatracurium compounds, e.g., cisatracurium besylate, from isoquinolinium salts of the structural formula (VIIA) wherein X? is an anion and R is H or a C1-C6 alkyl, or an activated form of the carboxylic acid with 1,5-pentanediol to form a cisatracurium salt, optionally via an intermediate compound (VIII). The cisatracurium compounds can be purified using simple techniques to afford pure cisatracurium besylate without the need for HPLC purification.

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

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 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: Provided is a process for producing highly pure 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (imiquimod), which includes reacting 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline with a non-gaseous amine precursor. Also provided are methods for isolating highly pure imiquimod. Further provided are intermediates useful in the production of imiquimod, methods for producing such intermediates, and methods for obtaining imiquimod from such intermediates.

Abstract: The present invention provides novel intermediates, which preferably include 3-substituted, alkyl 2,2-difluoro-3-hydroxy-3-(2,2-dialkyldioxolan-4-yl)-propionate derivatives, and 3,5-disubstituted-2-deoxy-2,2-difluoro-1-oxo-D-ribose derivatives. The present invention also provides processes for producing such intermediates and processes for producing gemcitabine therewith.

Abstract: The present invention provides processes for preparing novel chemical substances that are useful as intermediates in the preparation of gemcitabine and processes for preparing gemcitabine therewith. Exemplary intermediates include mixtures of D-erythro and D-threo (3R- and 3S-) isomers of 3-(hydroxy)-2,2-difluoro-3-(2,2-dimethyldioxolan-4-yl)propionic acid salts. Also provided is a novel process for selectively isolating the D-erythro and D-threo isomers of the said salts in purities of at least about 95%, and processes of using them for preparing nucleoside analogs such as, e.g., gemcitabine and intermediates and analogs thereof.

Abstract: The present invention provides several improved processes for preparing aripiprazole, wherein the first step comprising reacting 7-HQ with a 1,4-disubstituted-butane in biphasic reaction mixture or in a single phase solvent to obtain a 7-(4-halobutoxy)-3,4-dihydro-(1H)-quinolinone (7-HBQ) and the second step comprising reacting the 7-HBQ and 1-(2,3-dichlorophenyl)piperazine or an acid addition salt thereof in a biphasic reaction medium containing water and a water-immiscible solvent to obtain aripiprazole. Also provided are methods of purifying the 7-HBQs and aripiprazole.

Abstract: The present invention provides improved processes for preparing the intermediate 7-hydroxy-3,4-dihydro-2(1H)-quinolinone (7-HQ), which may be used in preparing the drug aripiprazole. Among these processes are included three efficient processes for preparing 7-hydroxy-3,4-dihydro-2(1H)-quinolinone comprising reacting N-(3-methoxyphenyl)-3-chloropropionamide with AlCl3 using novel reaction conditions thus obtaining a substantially pure product, which may be used in the subsequent steps for obtaining aripiprazole without further purification.

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: 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.