Patent application number | Description | Published |
20100099887 | Process for the Preparation of Pure Anastrozole - A process for the preparation of anastrozole which comprises: a) brominating 3,5-bis(2-cyanoprop-2-yl)toluene (II) in an organic solvent using a brominating agent to obtain 3,5-bis(2-cyanoprop-2-yl)benzylbromide (III); b) heating the reaction mass of step a) to the reflux temperature of the organic solvent for a period of time no longer than 3 hours; c) isolating and purifying the bromo intermediate (III) using an organic solvent; d) alkylating the bromo intermediate in the presence of a base, optionally a phase transfer catalyst, a 1,2,4-triazole and an organic solvent to obtain anastrozole; and e) isolating and purifying the anastrozole from an organic solvent. | 04-22-2010 |
20100113526 | Process for the Preparation of Esomeprazole Magnesium Dihydrate - A process for preparing Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate, processes for preparing various intermediates useful in the preparation of Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate and a novel polymorphic Form II of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]thio]-1H-benzimidazole. | 05-06-2010 |
20100113790 | Process for Preparing Isomers of Carmoterol - A process for preparing a compound of formula (III) comprising condensing an oxiranyl compound of formula (I) with an amine of formula (II) or a salt thereof wherein: R | 05-06-2010 |
20100113804 | Process for Preparing Dorzolamide - There is provided a process for preparing dorzolamide and processes for preparing intermediates useful in the preparation of dorzolamide. In particular, there is provided a process for preparing an acetoamido sulfone of formula (viii) comprising oxidation of a hydroxysulfonamide of formula (vii) in the presence of an oxidizing agent selected from the group consisting of: a peracid, tert-butyl hydroperoxide, dimethyl dioxirane, selenium dioxide, m-phenanthroline di-N-oxide, nitric acid and hydrogen peroxide. There is also provided a process for preparing an acetoamidosulfone of formula (ix-a) comprising converting a hydroxy sulfone of formula (viii) to the acetoamidosulfone of formula (ix-a) in the presence of acetonitrile and an acid. There is also provided a process for separating the cis- and trans-isomers of dorzolamide from a mixture of the trans-isomer of dorzolamide and the cis-isomer of dorzolamide comprising reacting the mixture of isomers with a carboxylic acid. | 05-06-2010 |
20100204493 | Process for the Preparation of Escitalopram - The present invention provides a novel process for the preparation of a compound of Formula III, and novel processes for preparing escitalopram using the compound of Formula III. | 08-12-2010 |
20110054218 | Process for the Synthesis of Propargylated Aminoindan Derivatives - A process for preparing a compound of formula (V) or its enantiomer, which comprises:
| 03-03-2011 |
20120165524 | Process for Preparing Levosimendan and Intermediates for Use in the Process - In an embodiment, the present invention provides a process for preparing (−)-6-(4-aminophenyl)-5-methylpyridazin-3-(2H)-one, which process comprises: a) reacting racemic 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone of formula II | 06-28-2012 |
Patent application number | Description | Published |
20090270633 | Synthesis of 4-[1-(4-cyano phenyl)-(1,2,4-triazol-1-yl)methyl] benzonitrile and 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile intermediate - The present invention relates to a process for the preparation of 4-[1-(4-cyano phenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile (letrozole), substantially free from its isomeric impurity. The preparation involves reaction of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile with 4-fluorobenzonitrile in the presence of an organic solvent and a silicon amine. The present invention also relates to a process for the preparation of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile which involves: (a) the reaction of a 4-halomethyl benzonitrile with 1,2,4-triazole in the presence of cesium carbonate and an organic solvent to obtain a reaction mass comprising 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile of formula II; and (b) precipitation of 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile (II) from the reaction mass using a suitable organic solvent. | 10-29-2009 |
20090326028 | Process for the preparation of temozolomide and analogs - A process for the preparation of compounds of formula IA, where R═CH | 12-31-2009 |
20100075999 | Process for the Preparation of Ethyl-N-(2,3-Dichloro-6-Nitrobenzyl)Glycine Hydrochloride - The invention relates to a process for the preparation of anagrelide, and for the preparation of intermediates for use in preparing anagrelide. The invention also relates to the intermediates per se, in particular compounds of Formula (V): | 03-25-2010 |
20100152229 | Process for the Synthesis of Moxifloxacin Hydrochloride - A new polymorph of moxifloxacin hydrochloride is described, together with a method for making the polymorph. In addition, new intermediates in the formation of moxifloxacin hydrochloride are described, having formulas (1) and (II): | 06-17-2010 |
20100160643 | Process for Preparing Trityl Olmesartan Medoxomil and Olmesartan Medoxomil - A process for the preparation of trityl olmesartan comprising (a) condensing 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazol-5-carboxylic acid alkyl ester with trityl biphenyl bromide in the presence of a polar aprotic solvent and a base selected from the group consisting of alkali metal carbonates, alkali metal hydroxides, alkali metal alkoxides, and tertiary amines to obtain a compound of formula V, | 06-24-2010 |
20110015394 | Method of Synthesis of Bosentan, Its Polymorphic Forms and Its Salts - The present invention relates to alkaline earth metal salts of bosentan, anyhdrous bosentan, polymorphic forms thereof, amorphous bosentan and processes for preparing them. The present invention further relates to a process for the preparation of bosentan and its pharmaceutically acceptable salts. | 01-20-2011 |
20110112292 | Crystalline Form of Tenofovir Disoproxil and a Process for Its Preparation - Crystalline Form C of tenofovir disoproxil, salts thereof and a process for its preparation. The process involves adding a solution comprising tenofovir disoproxil and an organic solvent to salt-saturated water, whereby the crystalline Form C of tenofovir disoproxil precipitates. The crystalline Form C of tenofovir disoproxil may be converted to a salt thereof. There is also provided a process for purifying a crude product comprising tenofovir monoisoproxil and tenofovir disoproxil. | 05-12-2011 |
20130029945 | Darunavir Polymorph and Process for Preparation Thereof - There is disclosed crystalline darunavir hydrate substantially free of any non-aqueous solvent. | 01-31-2013 |
20130150587 | Process for the Preparation of Esomeprazole Magnesium Dihydrate - A process for preparing Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate, processes for preparing various intermediates useful in the preparation of Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate and a novel polymorphic Form II of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]thio]-1H-benzimidazole. | 06-13-2013 |
20130150588 | Salts and Polymorphs of Dexrabeprazole - The present invention provides dexrabeprazole magnesium hydrate and a process for its preparation. The present invention also provides a magnesium, calcium or potassium salt of dexrabeprazole, optionally in amorphous form, and processes for its preparation. | 06-13-2013 |
20130160761 | Pharmaceutical Aerosol Composition - A pharmaceutical aerosol composition comprising at least one hydrofluoroalkane propellant; at least one active agent complexed with an adjuvant; and, optionally, at least one pharmaceutically acceptable excipient. | 06-27-2013 |
20130165686 | Process for the Preparation of Nateglinide - The present invention relates to a process for the preparation of substantially pure nateglinide of formula (I), substantially free from the cis-isomer and L-enantiomer and preparation of enantiomerically pure nateglinide form B, directly from the hydrolysis of a (−)-N-(trans-4-isopropylcyclohexyl-1-carbonyl)-D-phenylalanine alkyl ester in a ketonic solvent or water or mixture thereof. | 06-27-2013 |
20150037275 | RIFAXIMIN COMPLEXES - There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex and therapeutic uses of the complex. | 02-05-2015 |
20150045382 | RIFAXIMIN COMPLEXES - There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex and therapeutic uses of the complex. | 02-12-2015 |
20150080579 | Salts and Polymorphs of Dexrabeprazole - The present invention provides dexrabeprazole magnesium hydrate and a process for its preparation. The present invention also provides a magnesium, calcium or potassium salt of dexrabeprazole, optionally in amorphous form, and processes for its preparation. | 03-19-2015 |
20150141383 | Darunavir Polymorph and Process for Preparation Thereof - There is disclosed crystalline darunavir hydrate substantially free of any non-aqueous solvent. | 05-21-2015 |
Patent application number | Description | Published |
20120157544 | Process for the Preparation of O-Desmethyl Venlafaxine and Intermediate for Use Therein - The present invention relates to a compound of formula A, wherein R is alkyl. | 06-21-2012 |
20150246935 | Process for Preparing of Bortezomib - The present invention provides improved processes for the preparation of Bortezomib, tert-butyl[1-({(1S)-3-methyl-1-[(3aS,4S,6S,7aS)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl}amino)-1-oxo-3-phenylpropan-2-yl]carbamate of formula (IV) and N-{(1S)-3-methyl-1-[(3aS,4S,6S,7aS)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl} phenylalanine of formula (V). Compound (IV) is prepared by coupling (1R)-3-methyl-1-[(3aS,4S,6S,7aR)-3a,5,5-trimethyl-hexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butan-1-amine of formula (II) or its salt with N-(tert-butoxycarbonyl)-L-phenylalanine of formula (III) in a first solvent in the presence of a first coupling agent and a first base, wherein the coupling process does not comprise solvent exchange. Compound (V) is prepared by deprotecting compound (IV) using an alcoholic solution of an inorganic acid. | 09-03-2015 |
20150291639 | Antiviral Phosphonate Analogues and Process for Preparation Thereof - The present invention provides a compound of the Formula (I) | 10-15-2015 |
Patent application number | Description | Published |
20080234492 | Process for the Preparation of Carvedilol - A process for the preparation of carvedilol of formula (I) (I) either in enantiomeric substantially pure form, or as an enantiomeric mixture, optionally as a pharmaceutically acceptable salt thereof, which process comprises reacting 2,3-eopxypropoxy carbazole of formula (II) (II) or the R or S enantiomer thereof, with N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) (V) to yield benzyl carvedilol of formula (VI) (VI) which is debenzylated by catalytic hydrogenation to yield carvedilol of formula (I), either in enantiomeric substantially pure form, or as an enantiomeric mixture, and if desired reacting the thus formed carvedilol of formula (I) with an inorganic or organic acid to yield a pharmaceutically acceptable salt thereof, and/or, if desired, separating the enantiomers. The above process is characterised in that reaction of said 2,3-epoxypropoxy carbazole of formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) is carried out in water as the reaction medium. The present invention further provides carvedilol of formula (I) prepared by a process as described above, and pharmaceutical compositions containing the same and therapeutic uses thereof. | 09-25-2008 |
20090069574 | Process for the synthesis of an ace inhibitor - A process for the synthesis of trandolapril which comprises condensing N-[I-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride with trans octahydro-1H-indole-2-carboxylic acid in a first organic solvent comprising a water immiscible inert organic solvent and in the presence of a base, and isolating trandolapril from a second organic solvent. N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride may also be condensed with (2S,3aR,7aS) octahydro-1H-indole-2-carboxylic acid in a first organic solvent and in the presence of a base, and trandolapril isolated. There is also provided a process for the resolution of racemic trans octahydro-1H-indole-2-carboxylc acid. | 03-12-2009 |
20090137648 | PROCESS FOR THE PREPARATION OF IRBESARTAN HYDROCHLORIDE - The present invention is concerned with a process for the preparation of 2n-butyl-4-spirocyclopentane-1-[(2′-(tetrazol-5-yl)biphenyl-4-yl)methyl]-2-imidazolin-5-one hydrochloride, irbesartan hydrochloride, novel hydrated and anhydrous crystalline forms thereof, amorphous irbesartan hydrochloride, formulations containing the same, therapeutic uses thereof and methods of treatment employing the same. The process of the present invention is a one-pot process which comprises reacting intermediate compounds 2n-butyl-1,3-diazaspiro[4,4]non-1-en-4-one and 5-(4′-bromomethyl-biphenyl-2-yl)-1-trityl-1H-tetrazole. | 05-28-2009 |
20090187020 | Process And Intermediate For Preparation Of Donepezil - The invention relates to new compounds of formula (III): | 07-23-2009 |
20090221830 | Fexofenadine Polymorphs and Processes of Preparing the Same - Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical compositions thereof, therapeutic uses thereof and methods of treatment therewith. | 09-03-2009 |
20090263333 | Pharmaceutical compounds and compositions - The invention provides three polymorphic forms of crystalline levosalbutamol sulphate designated herein as Forms I, II and III. Crystalline levosalbutamol sulphate Form I is characterised by a powder XRD pattern with peaks at 10.8, 11.9, 13.0, 18.3, 28.5±0.2 degrees 2 theta. Crystalline levosalbutamol sulphate Form II is characterised by a powder XRD pattern with peaks at 8.7, 9.6, 15.2, 15.7, 19.1, 27.2, 30.7±0.2 degrees 2 theta. Crystalline levosalbutamol sulphate Form III is characterised by a powder XRD pattern with peaks at 5.5, 6.9, 7.3, 18.7±0.2 degrees 2 theta. Processes for making the new polymorphic forms and pharmaceutical compositions comprising them are also provided. A pharmaceutical composition comprises a therapeutically effective isomer of salbutamol or a salt, solvate, ester, derivative or polymorph thereof, a glucocorticoid and a pharmaceutically acceptable carrier or excipient and optionally one or more other therapeutic agents. Preferably the composition is an aerosol formulation comprising the drugs, a propellant and optionally one or more other ingredients, such as a surfactant, cosolvent, or bulking agent. Alternatively, DPI or inhalation suspensions may be used. | 10-22-2009 |
20090312357 | Rifaximin - Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa. | 12-17-2009 |
20110166237 | Process for the Synthesis of Arformoterol - The present invention provides a process for preparing a compound of formula (VI) or a salt thereof, the process comprising: (i) reacting 4-methoxyphenyl acetone with an amine of formula (VIII) under conditions of reductive amination to produce a compound of formula (II) or a salt thereof, wherein there is no isolation of an imine intermediate formed during the reductive amination; (ii) condensing the compound (II) or the acid addition salt thereof with an α-haloketone of formula (III) to produce the compound of formula (IV); (iii) reducing the compound (IV) to a compound of formula (V); and (iv) reducing the compound (V) to the compound of formula (VI), wherein the reduction is carried out in the presence of either (1) a hydrogen donating compound in the presence of a hydrogen transfer catalyst; or (2) ammonium formate using a hydrogenation catalyst, wherein R | 07-07-2011 |
20110184174 | Processes for the Synthesis of Levocetirizine and Intermediates for Use Therein - The present invention provides a compound of formula (IV) | 07-28-2011 |
20110207938 | Process for the Preparation of Rufinamide - The present invention relates to a process for the preparation of rufinamide of formula I, which process comprises: (i) reacting a 2,6-difluorobenzylhalide of formula II, wherein X is chloride, bromide or iodide, with an azide to obtain 2-(azidomethyl)-1,3-difluorobenzene of formula III; (ii) reacting 2-(azidomethyl)-1,3-difluorobenzene of formula III with methyl propiolate to obtain methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid of formula IV; and (iii) reacting methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid of formula IV with ammonia to obtain rufinamide of formula I. | 08-25-2011 |
20110245499 | Process for Resolving Zopiclone - The present invention provides a process for the preparation of the dextrorotatory isomer of zopiclone (eszopiclone). The present invention also provides eszopiclone di-p-anisolyl-L-tartrate and eszopiclone diacetyl-L-tartrate, which are useful as intermediates in a process for preparing eszopiclone. | 10-06-2011 |
20110257418 | Process for Preparing Zanamivir and Intermediates for Use in the Process - The present invention provides a process for preparing methyl 5-acetamido-4-amino-6-(1,2,3-triacetoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylate (V), which process comprises reducing methyl 5-acetamido-4-azido-6-(1,2,3-triacetoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylate (IV) in the presence of a reducing agent selected from the group consisting of lithium aluminium hydride, sodium borohydride, zinc/ammonium chloride, zinc-ferric chloride and ferric chloride/sodium iodide. The present invention also provides compounds of formula (VIII) and (IX) which may be used in the synthesis of zanamivir. The present invention also provides processes for preparing compounds (VIII) and (IX) and processes involving their use, including in the synthesis of zanamivir. | 10-20-2011 |
20110262378 | Rifaximin Complexes - There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex, and therapeutic uses of the complex. | 10-27-2011 |
20120041199 | Process for the Preparation of Doxazosin and Salts Thereof - The present invention relates to a process for the preparation of doxazosin or salts thereof. | 02-16-2012 |