Class / Patent application number | Description | Number of patent applications / Date published |
549074000 | Nitrogen attached indirectly to the hetero ring by nonionic bonding | 47 |
20090275760 | PROCESS FOR THE PREPARATION OF PURE DULOXETINE HYDROCHLORIDE - The present invention relates to a process for the preparation of pure Duloxetine hydrochloride. The present invention further relates to duloxetine hydrochloride substantially free of residual hydrochloric acid. | 11-05-2009 |
20120029211 | Catalytic Wittig and Mitsunobu Reactions - A catalytic Wittig method utilizing a phosphine including the steps of providing a phosphine oxide precatalyst and reducing the phosphine oxide precatalyst to produce the phosphine; forming a phosphonium ylide precursor from the phosphine and a reactant; generating a phosphonium ylide from the phosphonium ylide precursor; reacting the phosphonium ylide precursor with the aldehyde, ketone, or ester to form the olefin and the phosphine oxide which then reenters the cycle. The invention is also directed to a Mitsunobu reaction catalytic in phosphine. | 02-02-2012 |
20150119582 | NAPHTHYL-CONTAINING COMPOUNDS FOR LIGHT-EMITTING DEVICES - Naphthyl-containing compounds having structural formula S | 04-30-2015 |
20160137587 | TRANSITION-METAL-FREE N-ARYLATION OF TERTIARY AMINES USING ARYNES - The present invention relates to transition-metal-free process for the synthesis of tertiary arylamines comprises coupling reaction between arynes and N,N-dimethyl aniline compounds in presence of 18-crown-6, KF and THF. | 05-19-2016 |
549075000 | Chalcogen attached indirectly to the hetero ring by nonionic bonding | 43 |
20080207923 | Pure DNT-maleate and methods of preparation thereof - (S)—N,N-Dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine maleate (DNT-maleate) and polymorphs of DNT-maleate, compositions of DNT-maleate and its polymorphs, processes for the preparation of DNT-maleate and its polymorphs, and processes for the preparation of duloxetine hydrochloride from DNT-maleate are provided. Processes for preparing chemically pure duloxetine and chemically pure duloxetine intermediates are also provided. In addition, chemically pure DNT and salts thereof are provided. | 08-28-2008 |
20080287693 | Process for the Preparation of 1-Naphthol Mixed Ethers and Intermediates of Crystalline Forms of (+) and (-)-Duloxetine - The invention relates to a process for the preparation of duloxetine (1a), comprising the reaction between 1-fluoronaphthalene and 3-N,N-dimethylamino-1-(2-thienyl)-propan-1-ol in the presence of 1,3-dimethyl-2-oxo-hexahydropyrimidine (DMPU) as the solvent; a method for the identification of duloxetine enantiomers and for the determination of its optical purity is also disclosed. | 11-20-2008 |
20080293952 | Method for the Preparation of (S)-N-Methyl-3-(1-Naphthyloxy)-3-(2-Thienyl)Propylamine Hydrochloride (Duloxetine) - A method of preparation of (S)—N-methyl-3-(1-naphthyloxy)-3-(2-mienyl)propylamine of Formula (I) and its pharmaceutically acceptable salts, comprising a) reaction of (RS)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with optically active D-tartaric acid or an acid salt derived from D-tartaric acid forming a mixture of diastereoisomeric salts of N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine and D-tartaric acid (2:1), b) isolation of the salt (S)—N,N-dimethyl-3-(naphthyloxy)-3-(2-thienyl)propylamine/D-tartrate (2:1) from the mixture of diastereoisomeric salts in an organic solvent, water or a mixture thereof and release of (S)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine by action of an inorganic or organic base, c) demethylation of (S)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine by action of an alkylchloroformate of formula ClCOOR (R=C | 11-27-2008 |
20090082580 | COMPOSITIONS AND METHODS FOR STORING HOLOGRAPHIC DATA - In one aspect, the present invention provides a novel thiophene-containing polynitrone compound having structure (II) | 03-26-2009 |
20090093645 | SYNTHESIS AND PREPARATIONS OF DULOXETINE SALTS - The invention relates to an improved process for the preparation of duloxetine hydrochloride. | 04-09-2009 |
20090112000 | METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF 3-METHYLAMINO-1-(2-THIENYL)PROPAN-1-OL - The present invention provides a methylhydroxylaminopropanol derivative and the methylhydroxylaminopropanol derivative of the present invention is used as an intermediate for preparation of 3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (+)-(S)—N-methyl-3-methyl-3-( | 04-30-2009 |
20090112001 | OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF (S)-(-)-3-METHYLAMINO-1-(2-THIENYL)PROPAN-1-OL - The present invention provides an (S)-methylhydroxylaminopropanol derivative and the (S)-methylhydroxylaminopropanol derivative of the present invention is used as an intermediate for preparation of (S)-(−)-3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing (S)-(−)-3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol derivative is used as an intermediate. | 04-30-2009 |
20090143600 | METHOD OF MANUFACTURING (S)-N-METHYL-3-(1-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE HYDROCHLORIDE (DULOXETINE) - A method of preparation of (S)—N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (I) or its pharmaceutically acceptable salt, in which (RS)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (III) is reacted with an optically active acid, after which a crystallization is made of that diastereoisomer which yields, by reaction with an inorganic or organic base, (S)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (S)-III, which is then demethylated using alkylchloroformates, followed by a hydrolysis and optional conversion of the compound of formula (I) to its salt. | 06-04-2009 |
20100069649 | METHOD OF PURIFICATION OF (S)-N-METHYL-3-(1-NAPHTYLOXY)-3-(2-THIENYL) PROPYLAMINE HYDROCHLORIDE (DULOXETINE) - A method of purification of (5)-7V-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine hydrochloride of formula I, comprising (a) transformation of the substance of formula I to its free base by the action of an organic or inorganic base in an aqueous environment; and (b) transformation of the base of the substance of formula I to crystalline hydrochloride by the action of hydrochloric acid or gaseous HCl in an organic solvent or a mixture of organic solvents. A method of purification of (S)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine hydrochloride of formula I, comprising dissolution of this substance in a minimum quantity of methanol containing 0 to 50% of water and its transformation back to the solid phase (precipitation) by addition of a less polar solvent. | 03-18-2010 |
20100105925 | NOVEL PROCESS FOR PREPARATION OF DULOXETINE HYDROCHLORIDE - An improved process for synthesis of duloxetine hydrochloride (1) having chiral purity greater than 99.9% that is characterized by the following:
| 04-29-2010 |
20100222602 | CRYSTALLINE ROTIGOTINE BASE AND PREPARATION PROCESS THEREFOR - An isolated and pure crystalline rotigotine base of polymorph Form I, and processes for producing the crystalline rotigotine base are disclosed. Also disclosed is a transdermal patch for the delivery of rotigotine base using the disclosed isolated and pure form of rotigotine base, which can be used in treatment of Parkinson's Disease and other disorders ameliorated or treated by rotigotine, including restless leg syndrome. | 09-02-2010 |
20100234619 | PREPARATION OF (S)-(+)-N-METHYL-3-(1-NAPHTHYLOXY)-3-(2-THIENYL) PROPYLAMINE USING OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AS AN INTERMEDIATE - The present invention provides a (S)-methylhydroxylaminopropanol derivative as an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine. The present invention also provides a process for preparing (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol derivative is used as an intermediate. | 09-16-2010 |
20100234620 | PROCESS FOR PREPARING N-METHYL-N-HYDROXYL-3-(1-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE DERIVATIVE - The present invention provides a process for preparing a N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound. The present invention also provides a process for preparing (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with higher yield and low treatment cost, which includes the preparation of the N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound. | 09-16-2010 |
20100267968 | METHOD FOR THE PREPARATION OF DULOXETINE HYDROCHLORIDE - The present invention relates to an improved process for the preparation of Duloxetine and its intermediates (S)-(+)-N,N-dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine by reacting (S)-(+)-N,N-dimethyl-3-(2-thienyl)-3-hydroxypropanamine with 1-fluoronaphthalene in the presence of a base; wherein the improvement lies in conducting the reaction in the absence of solvent. | 10-21-2010 |
20100286412 | SYNTHESIS AND PREPARATIONS OF DULOXETINE SALTS - The invention relates to an improved process for the preparation of duloxetine, duloxetine intermediates, and duloxetine hydrochloride. | 11-11-2010 |
20110137049 | CHIRAL IRIDIUM AQUA COMPLEX AND METHOD FOR PRODUCING OPTICALLY ACTIVE HYDROXY COMPOUND USING THE SAME - The invention provides a chiral iridium aqua complex which has good preservation stability, can be easily produced, and enables asymmetric transfer hydrogenation in a higher yield and with higher stereoselectivity. The chiral iridium aqua complex has the formula (1A): | 06-09-2011 |
20110152543 | PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE (S)-(-)-2-(N-PROPYLAMINO)-5-METHOXYTETRALINE AND (S)-(-)-2-(N-PROPYLAMINO)-5-HYDROXYTETRALINE COMPOUNDS - The present invention describes a novel process for the preparation of optically active (S)-(−)-2-(N-propylamino)-5-methoxytetraline and (S)-(−)-2-(N-propylamino)-5-hydroxytetraline compounds based on the optical resolution of mixtures of the enantiomers of 2-(N-propylamino)-5-methoxytetraline and 2-(N-propylamino)-5-hydroxytetraline respectively. This process comprises (a) reacting a mixture of the enantiomers of said compounds with an optically active organic acid to form diastereoisomeric salts and separating the salts by crystallization. Said compounds are useful in the preparation of (6S)-(−)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine). Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson's disease. | 06-23-2011 |
20110207946 | Process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols - Provided is a process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols, particularly of (S)-(−)- and (R)-(+)-3-N-methylamino-1-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of formula (II), wherein R | 08-25-2011 |
20110230666 | PROCESS FOR THE SEPARATION OF ENANTIOMERICALLY PURE COMPOUNDS - The present patent application relates to an improved process for the separation of enantiomerically pure compounds. Specifically it relates to separation of enantiomerically enriched Rivastigmine, Duloxetine, Escitalopram and their intermediates in high yields. | 09-22-2011 |
20110275836 | PROCESS FOR THE PREPARATION OF DULOXETINE AND SALTS THEREOF - The present invention relates to improved process for the preparation of Duloxetine of formula (I) and salts thereof wherein said improvement takes place in step of condensation. | 11-10-2011 |
20110306776 | PROCESS FOR THE PREPARATION OF (6S)-(-)-5,6,7,8-TETRAHYDRO-6-[PROPYL-(2-THIENYL)ETHYL]AMINO-1-NAPHTHOL (ROTIGOTINE) - The present invention describes a novel process for the preparation of (6S)-(−)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine) comprising: (a) acetylating (S)-(−)-5-hydroxy-N-n-propyl-2-aminotetraline to afford the acetate; (b) reacting this acetate, (−)-5-acetoxy-N-n-propyl-2-aminotetraline, with 2-(2-thienyl)ethanol 2-nitrobenzenesul-fonate; (d) hydrolyzing (6S)-(−)-1-acetoxy-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthalene to afford (6S)-(−)-5,6,7,8-tetrahydro-6-[propyl-(2-thienypethyl]amino-1-naphthol (Rotigotine) and (d) purifying rotigotine either by the acetylation reaction and subsequent hydrolysis of the formed acetate or by salification of rotigotine through hydrochloride or hydrobromide formation and subsequent base release. Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson's disease. | 12-15-2011 |
20110313176 | PROCESSES FOR PREPARING HIGHLY PURE ROTIGOTINE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Provided herein are convenient, industrially advantageous and environmentally friendly processes for the preparation of (−)-(S)-5-hydroxy-2-[N-n-propyl-N-2-(2-thienyl)ethylamino]tetralin (rotigotine) or a pharmaceutically acceptable salt thereof. Provided further herein is a highly pure rotigotine or a pharmaceutically acceptable salt thereof substantially free of impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure rotigotine or a pharmaceutically acceptable salt thereof substantially free of impurities. | 12-22-2011 |
20120029212 | METHOD FOR THE PREPARATION OF (S)-N-METHYL-3-(1-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE HYDROCHLORIDE (DULOXETINE) - A method for the preparation of a duloxetine hydrochloride salt from a duloxetine base, comprising the steps of: reacting duloxetine base with concentrated hydrochloric acid in ethylmethylketone; and crystallizing duloxetine hydrochloride salt from said concentrated hydrochloric acid in ethylmethylketone. | 02-02-2012 |
20120095239 | A PROCESS FOR THE PREPARATION OF DULOXETINE HYDROCHLORIDE - The present invention relates to a process for the preparation of Duloxetine hydrochloride of formula (I). | 04-19-2012 |
20120190869 | OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF (S)-(-)-3-METHYLAMINO-1-(-2-THIENYL)PROPAN-1-OL - The present invention provides an (S)-methylhydroxylaminopropanol compound and the (S)-methylhydroxylaminopropanol compound of the present invention is used as an intermediate for preparation of (S)-(−)-3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing (S)-(+3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol compound is used as an intermediate. | 07-26-2012 |
20130005992 | METHOD FOR PRODUCING OPTICALLY ACTIVE N-MONOALKYL-3-HYDROXY-3-ARYLPROPYLAMINE COMPOUND - The present invention provides a method for producing an N-monoalkyl-3-hydroxy-3-arylpropylamine compound represented by Formula (2): | 01-03-2013 |
20130096321 | CRYSTALLINE ROTIGOTINE BASE AND PREPARATION PROCESS THEREFOR - An isolated and pure crystalline rotigotine base of polymorph Form I, and processes for producing the crystalline rotigotine base are disclosed. Also disclosed is a transdermal patch for the delivery of rotigotine base using the disclosed isolated and pure form of rotigotine base, which can be used in treatment of Parkinson's Disease and other disorders ameliorated or treated by rotigotine, including restless leg syndrome. | 04-18-2013 |
20130102794 | Novel Process for the Preparation of Nitrogen Substituted Aminotetralins Derivatives - The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R | 04-25-2013 |
20140005414 | PREPARATION OF DULOXETINE HYDROCHLORIDE USING OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL COMPOUND AS AN INTERMEDIATE | 01-02-2014 |
20140031564 | PROCESS FOR PREPARING (S)-3-N-METHYLAMINO-1-(2-THIENYL)-1-PROPANOL - The present invention relates to a method for preparing (S)-3-N-methylamino-1-(2-thienyl)-1-propanol and salts thereof. | 01-30-2014 |
20140357874 | PROCESS FOR PREPARING (S)-3-N-METHYLAMINO-1-(2-THIENYL)-1-PROPANOL - The present invention relates to a method for preparing (S)-3-N-methylamino-1-(2-thienyl)-1-propanol and salts thereof. | 12-04-2014 |
20150361064 | Process for the Preparation of N-Monosubstituted beta-Amino Alcohols - A process is disclosed for the preparation of a compound of formula | 12-17-2015 |
549076000 | The chalcogen, X, is in a -C(=X)- group | 11 |
20080262247 | Process for preparing arylaminopropanols - The invention relates to a process for preparing enantiomerically enriched arylaminopropanols and to their use and also to intermediates. | 10-23-2008 |
20100298576 | ASYMMETRIC CYCLIZATION PROCESSES USING UNSATURATED NITRO COMPOUNDS - Disclosed are processes of forming a compound (33), (35) or (37) | 11-25-2010 |
20110004007 | PROCESS FOR THE PREPARATION OF N-MONOSUBSTITUTED beta-AMINO ALCOHOLS - A process is disclosed for the preparation of a compound of formula | 01-06-2011 |
20140018549 | USE OF D-SERINE DERIVATIVES FOR THE TREATMENT OF ANXIETY DISORDERS - Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias, wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R | 01-16-2014 |
20150119583 | CATALYST FOR ORGANIC REACTION AND METHOD OF USE THEREOF - A catalyst for an organic reaction and a method of using a catalyst in an organic reaction are provided. The catalyst for an addition or condensation reaction includes a graphene oxide including an oxygen functional group, and the catalyst is configured to promote the addition or condensation reaction by bonding the oxygen functional group with an alkali metal ion or alkali earth metal ion during the addition or condensation reaction. | 04-30-2015 |
549077000 | Unsaturated carbocyclic ring or acyclic carbon to carbon unsaturation containing | 6 |
20090012316 | Crystal forms of (S)-(+)-N,N-dimethyl-3-(1-Napathalenyloxy)-3-(2-thienyl)propanamine oxalate and the preparation thereof - DNT-Oxal crystalline forms and processes for making DNT-Oxal crystalline forms are provided. | 01-08-2009 |
20090286997 | PROCESS FOR PREPARING ARYLAMINOPROPANOLS - The invention relates to a process for preparing enantiomerically enriched aryl-aminopropanols and to their use and also to intermediates. | 11-19-2009 |
20120004424 | MICHAEL REACTION WITH RECOVERY OF THE CATALYST - Disclosed is a process of carrying out a Michael reaction with recovery of the catalyst, where a compound of formula (1): | 01-05-2012 |
20130046100 | S-5-SUBSTITUENT-N-2'-(THIOPHENE-2-YL)ETHYL-TETRALIN-2-AMINE OR CHIRAL ACID SALTS THEREOF AND USE FOR PREPARING ROTIGOTINE - The chiral compound S-5-substituted-N-2′-(thienyl-2-yl-)ethyl-tetralin-2-amine or its chiral acid salts and preparation method thereof are disclosed, and the method for preparing Rotigotine by using the chiral compound is also disclosed. Racemic 5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 1) is resolved by using a conventional chiral acid to obtain an optically pure chiral acid salt of S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 2). The compound 2 or chiral acid salt thereof is alkylated and deprotected to produce rotigotine (compound 5). | 02-21-2013 |
20130190514 | PHENYLALKYL N-HYDROXYUREAS FOR TREATING LEUKOTRIENE RELATED PATHOLOGIES - The method of treating patients by administering N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea for treatment of leukotriene related pathologies, and compositions for this use. | 07-25-2013 |
20140371469 | PHOTOREACTIVE BENZAMIDE PROBES FOR HISTONE DEACETYLASE 2 - The design, modeling, synthesis, biological evaluation, and photoaffinity labeling studies of a series of photoreactive potent and selective HDACs 1 and 2 benzamide based probes are disclosed herein. | 12-18-2014 |