Abstract: Disclosed herein are methods of obtaining highly pure 5-azacytidine, which contains minimal amounts of degradation impurities and methods of assessing the impurity profile of the degradation of cytidine analogues, such as 5-azacytidine

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: 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: Provided is a process for purifying a letrozole product that contains an isoletrozole impurity, which process preferably includes converting at least a portion of the isoletrozole impurity into 4,4?-dicyanobenzophenone and removing 4,4?-dicyanobenzophenone, to produce a purified letrozole product.

Abstract: Provided is a process for preparing gemcitabine or a salt thereof, which preferably includes selectively precipitating the ?-anomer of a 3?,5?-di-O-protected-N4-trimethylsilyl-2?-deoxy-2?,2?-difluorocytidine, removing the protecting groups to produce gemcitabine, and, optionally, converting the gemcitabine into a salt. Preferably, the 3? and 5? protecting groups are the same or different, and at least one of the 3? and 5? protecting groups is cinnamoyl, naphthoyl, naphthylmethylcarbonyl, 2-methylbenzylcarbonyl, 4-methylbenzylcarbonyl or 9-fluorenylmethyloxycarbonyl. Also provided are methods for enriching the ?-anomer from an anomeric mixture of a 3?,5?-di-O-protected-N4-trimethylsilyl-2?-deoxy-2?,2?-difluorocytidine, e.g., a N4-trimethylsilyl-2?-deoxy-2?,2?-difluoro-cytidine-3?,5?-diester, e.g., 3?,5?-dicinnamoyl-N4-trimethylsilyl-2?-deoxy-2?,2?-difluorocytidine, using a slurrying process, and methods for converting the ?-anomer-enriched product into gemcitabine or a salt thereof.

Abstract: Provided is a process for purifying a letrozole product that contains an isoletrozole impurity, which process preferably includes converting at least a portion of the isoletrozole impurity into 4,4?-dicyanobenzophenone and removing 4,4?-dicyanobenzophenone, to produce a purified letrozole product.

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: 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: 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: 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 (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 process for the preparation of 6,6-dimethylhept-1-en-4-yn-3-ol comprising of reacting t-butylacetylene with a proton-extracting agent selected from the group consisting of an organometallic compound and metallic lithium to form a t-butylacetylide, reacting the acetylide with acrolein at temperatures between −40° C. to +20° C., quenching the reaction mixture and isolating the product.

Abstract: The invention provides a process for the preparation of 6,6-dimethylhept-1-en-4-yn-3-ol comprising of reacting t-butylacetylene with a proton-extracting agent selected from the group consisting of an organometallic compound and metallic lithium to form a t-butylacetylide, reacting the acetylide with acrolein at temperatures between −40° C. to +20° C., quenching the reaction mixture and isolating the product.

Abstract: There are provided orally-administrable formulations for the controlled release of granulated garlic, comprising particles of granulated garlic coated with a film comprising a mixture of at least one water soluble polymer and at least one water insoluble polymer, said at least one water soluble polymer and at least one water insoluble polymer being present in a ratio that produces a substantially zero order linear release pattern of at least one active ingredient. Preferably, the formulations are characterized in that the total in vitro dissolution time of said formulations required for release of 75% of the Allicin available from said formulations based upon the total amount of alliin initially present in said formulations is between about 4 and about 12 hours, as determined by U.S.P. XXIII paddle method at a paddle speed of 150 rpm, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, containing 0.1% w/w sodium dodecyl sulfate (SDS), at pH 6.

Abstract: The present invention relates to controlled/extended release oral dosage forms of chromium picolinate. Chromium picolinate is a common and effective biologically active form of chromium. As such, it has beneficial nutritional and therapeutic effects including improved insulin metabolism and lipid lowering activity.The controlled dosage form of the present invention can be provided in various ways, including matrix formulations such as matrix tablets or multiparticulate formulations like micro capsules or coated pellets put into hard gelatin capsules. This provides effective drug delivery for extended periods of time, at relatively stable, optimal plasma peak values, with minimal undesirable side effects.The invention provides effective controlled/extended release oral dosage formulations of chromium picolinate and processes for their preparation.