Abstract: A novel process is disclosed for producing Imatinib, using the precursor 2-chloro-4-(3-pyridyl)-pyrimidine, thus improving Imatinib preparation via an alternative synthetic route, avoiding the use of the toxic reagent cyanamide.

Abstract: Provided is a process for producing highly pure midazolam and salts thereof, and a pharmaceutical composition containing the highly pure midazolam and/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 process for producing imatinib and salts thereof, e.g., imatinib mesylate. The process includes reacting4-(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: 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 crystalline granisetron base form I and processes for producing crystalline granisetron base form I, which is suitable for preparing, e.g., granisetron salts such as, e.g., the hydrochloride salt. Also provided is a process for producing a salt of granisetron from crystalline granisetron base form I.

Abstract: Provided herein is a spray dried stable amorphous imatinib mesylate as a free-flowing solid and process for producing the amorphous imatinib mesylate in highly pure form.

Abstract: Novel crystalline forms of Donepezil base, processes for producing same, pharmaceutical compositions containing same and methods of treatment utilizing same are disclosed.

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: The present invention is directed to a process of preparing montelukast or a salt thereof with minimal amounts of impurities, such as a dehydration impurity (compound (VI)) or a cyclic ether impurity (compound (VIII)).

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 for preparing 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (Imiquimod) of formula (I). The process comprises heating 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (II) with formamide, and optionally with bubbling of gaseous ammonia to afford Imiquimod of formula (I). According to the present invention, by using this process and novel purification methods, essentially as described herein, highly pure Imiquimod is obtained.

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 a process for purifying carbostyril derivatives such as 7-(4-bromobutoxy)-3,4-dihydro-2(1H)-quinolinone and 7-(4-chlorobutoxy)-3,4-dihydro-2(1H)-quinolinone and aripiprazole by passing a solution of the material in an organic solvent through a suitable absorbing material.

Abstract: Novel crystalline forms I, II, III, IV, V, VI, VII, VIII, IX, and X of montelukast ammonium salts are provided, and novel methods of making these forms are disclosed.

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: 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: 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 a process for preparing 4-amino-1-isobutyl-1H-imidazo[4,5-c]quinoline (Imiquimod) of formula (I). The process comprises heating 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline of formula (II) with formamide, and optionally with bubbling of gaseous ammonia to afford Imiquimod of formula (I). According to the present invention, by using this process and novel purification methods, essentially as described herein, highly pure Imiquimod is obtained.

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.