| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 544319000 | At 4- or 6-position | 50 |
| 20090043098 | Method for Preparation of Optionally 2-Substituted 1,6-Dihydro-6-Oxo-4-Pyrimidinecarboxylic Acids - A new method for the preparation of optionally 2-substituted 1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid compound of Formula 1 is disclosed | 02-12-2009 |
| 20090111984 | Novel Method For Producing Pyrimidine Compound | 04-30-2009 |
| 20090281316 | PROCESS FOR THE PREPARATION OF SUBSTITUTED CYANOPHENOXY-PYRIMIDINYLOXY-PHENYL ACRYLATE DERIVATIVES - The present invention provides a process for reacting between a phenol derivative and an aromatic substrate under phenolate forming conditions comprising the following steps: (a) reacting a phenol derivative with a base in a polar organic solvent to obtain a phenolate salt, wherein water is removed form the reaction mixture during the reaction, (b) adding the aromatic substrate to the reaction mixture obtained in step (a), (c) heating the reaction mixture of step (b) to a temperature in the range of 80° to 1300° C., preferably, 90° to 1000° C. for 2 to 7 hours to obtain a phenoxy substituted aromatic substrate, (d) removing the solvent from the mixture of step (c) and optionally further isolating an purifying the phenoxy substituted aromatic substrate. Optionally, the removal of water during step (a) is in conjunction with partial removal of the organic solvent. | 11-12-2009 |
| 20100036124 | PREPARATION OF AZOXYSTROBIN - The present invention relates, inter alia, to a process for preparing a compound of formula (I): using, as a catalyst 1,4-diazabicyclo[2.2.2]octane. | 02-11-2010 |
| 20100081811 | METHOD FOR THE NITRATION OF 4,6-DIHYDROXY-2-METHYLPYRIMIDINE - Disclosed is a method for the nitration of 4,6-dihydroxy-2-methylpyrimidine for the synthesis of 4,6-dihydroxy-5,5-dinitro-2-(dinitromethylene)-2,5-dihydropyrimidine which is used as a precursor of 1,1-diamino-2,2-dinitroethylene, one type of explosives. The present invention provides an improved method for the nitration of 4,6-dihydroxy-2-methylpyrimidine, wherein organic solvent is applied in the nitration process of 4,6-dihydroxy-2-methylpyrimidine thereby solving the safety problem while improving the yield of nitration. | 04-01-2010 |
| 20100179320 | PREPARATION METHODS OF AZOXYSTROBIN AND ITS ANALOGS - Preparation method of a compound of general formula (I) comprises the following steps: (1) a compound of general formula (II) reacts with a formylating agent in an aprotic solvent at a temperature between −20° C. and 200° C. in the presence of a Lewis acid, then an organic base is added to promote the reaction to obtain an intermediate product; (2) the above intermediate product reacts with a methylating agent in the presence of an alkali at a temperature between −20° C. and 100° C. to obtain the compound of formula (I). | 07-15-2010 |
| 20100190983 | PROCESS FOR PREPARING VORICONAZOLE - Optically pure voriconazole can be prepared in a high yield by a) subjecting 1-(2,4-difluorophenyl)-2(1H-1,2,4-triazol-1-yl)ethanone to Reformatsky-type coupling reaction with a substituted thiopyrimidine derivative to obtain a desired (2R,3S)/(2S,3R)-enantiomeric pair; b) removing the thiol derivative from the enantiomer to obtain racemic voriconazole; and c) isolating the racemic voriconazole by way of optical resolution using an optically active acid. | 07-29-2010 |
| 20100204472 | Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation - This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation. | 08-12-2010 |
| 20100249410 | PROCESS FOR PREPARING N-ALKYLATED HYDROXYPYRIMIDINONE COMPOUNDS - Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: | 09-30-2010 |
| 20100280244 | PROCESS FOR PREPARING N-SUBSTITUTED HYDROXYPYRIMIDINONE CARBOXAMIDES - Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed. | 11-04-2010 |
| 20110178299 | OPTICALLY ACTIVE DIFLUOROMETHANESULFONANILIDE DERIVATIVE AND HERBICIDE - The present invention aims at providing an optically active difluoromethanesulfonanilide derivative exhibiting an excellent herbicidal activity at a low dose. | 07-21-2011 |
| 20120088914 | PRODUCTION METHOD OF PYRIMIDINE COMPOUNDS - 4-amino-6-alkynyloxypyrimidine compounds shown by the formula (V) | 04-12-2012 |
| 20120178930 | NOVEL POLYMORPHS OF RALTEGRAVIR POTASSIUM - The present invention provides novel polymorphs of raltegravir potassium, processes for their preparation and pharmaceutical compositions comprising them. Thus for example, raltegravir potassium was added to water and stirred for 15 minutes, the solution was filtered on hiflo bed and the bed washed with water, the resulting solution was subjected to freeze drying at −180 deg C. for 13 hours to give raltegravir potassium amorphous form. | 07-12-2012 |
| 20120178931 | PROCESS FOR PREPARATION OF PYRIMIDINYLACETONITRILE DERIVATIVES AND INTERMEDIATES FOR SYNTHESIS THEREOF - Provided is a process by which pyrimidinylacetonitrile derivatives can be prepared easily and efficiently from industrially available raw materials. Also provided are intermediates for the synthesis of the derivatives. A process for the preparation of pyrimidinylacetonitrile derivatives represented by general formula (3) [wherein X is a halogen atom, and R is an alkoxymethyl group], characterized by reacting a 2,4-dihalogeno-6-nitrobenzene derivative represented by general formula (1) [wherein X and R are each as defined above] with 4,6-dimethoxy-2-cyanomethylpyrimidine represented by general formula (2) [wherein Me represents a methyl group] in the presence of a base; and intermediates for the synthesis of the pyrimidinylacetonitrile derivatives. | 07-12-2012 |
| 20120190851 | METHOD FOR PRODUCING 4,6-DIALKOXY-2-CYANOMETHYLPYRIMIDINE AND SYNTHETIC INTERMEDIATE THEREOF - Disclosed is a method for producing 4,6-dialkoxy-2-cyanomethylpyrimidine and also disclosed is a synthetic intermediate thereof. More specifically disclosed is a method for producing 4,6-dialkoxy-2-cyanomethylpyrimidine represented by general formula (2) (wherein R represents an alkyl group), comprising reacting a t-butyl cyanoacetate derivative represented by general formula (1) (wherein R has the same meaning as described above) in the presence of an acid, and also disclosed is a t-butyl cyanoacetate derivative represented by general formula (1) (wherein R represents an alkylgroup). | 07-26-2012 |
| 20120232271 | METHOD FOR PREPARATION OF OPTIONALLY 2-SUBSTITUTED 1,6-DIHYDRO-6-OXO-4-PYRIMIDINECARBOXYLIC ACIDS - A new method for the preparation of optionally 2-substituted 1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid compounds of Formula 1 is disclosed | 09-13-2012 |
| 20130005973 | PROCESS FOR PREPARING VORICONAZOLE BY USING NEW INTERMEDIATES - Provided is a process for preparing Voriconazole represented by Chemical Formula 1. More particularly, the process for preparing Voriconazole of Chemical Formula 1 includes: carrying out the Reformatsky-type coupling reaction between a ketone derivative of Chemical Formula 4 and a pyrimidine derivative of Chemical Formula 5 to obtain a compound of Chemical Formula 3; reacting the substituents halo and oxysulfonyl with a hydrogen donor to obtain racemic Voriconazole of Chemical Formula 2; and carrying out optical isolation of the racemic Voriconazole by adding an adequate optically active acid thereto to obtain Voriconazole having high optical purity with high cost-efficiency and high yield. | 01-03-2013 |
| 20130137868 | SALTS OF RALTEGRAVIR - The present invention provides novel salts of raltegravir, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides crystalline sodium salt of raltegravir, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a process for the preparation of amorphous sodium salt of raltegravir. The present invention further provides a process for the preparation of raltegravir potassium crystalline form H | 05-30-2013 |
| 20130172557 | 2,6-DIHALO-5-ALKOXY-4-SUBSTITUTED-PYRIMIDINES, PYRIMIDINE- CARBALDEHYDES, AND METHODS OF FORMATION AND USE - 2,6-Dihalo-5-alkoxy-4-substituted-pyrimidines, 2,6-dihalo-5-alkoxy-4-pyrimdine carbaldehydes, and derivatives of each are useful intermediates in forming potent herbicides that demonstrate a broad spectrum of weed control. These compounds are disclosed, as are methods of forming and using these compounds. | 07-04-2013 |
| 20130261303 | PROCESS FOR THE PREPARATION OF SUBSTITUTED CYANOPHENOXY-PYRIMIDINYLOXY-PHENYL ACRYLATE DERIVATIVES - The present invention provides a process for reacting between a phenol derivative and an aromatic substrate under phenolate forming conditions comprising the following steps: (a) reacting a phenol derivative with a base in a polar organic solvent to obtain a phenolate salt, wherein water is removed from the reaction mixture during the reaction, (b) adding the aromatic substrate to the reaction mixture obtained in step (a), (c) heating the reaction mixture of step (b) to a temperature in the range of 80° to 1300° C., preferably, 90° to 1000° C. for 2 to 7 hours to obtain a phenoxy substituted aromatic substrate, (d) removing the solvent from the mixture of step (c) and optionally further isolating and purifying the phenoxy substituted aromatic substrate. Optionally, the removal of water during step (a) is in conjunction with partial removal of the organic solvent. | 10-03-2013 |
| 20130303763 | METHODS AND COMPOSITIONS FOR THE TREATMENT OF NECROTIZING ENTEROCOLITIS - This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of necrotizing enterocolitis. | 11-14-2013 |
| 20140058104 | METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE - Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions. | 02-27-2014 |
| 20140155607 | Novel Salts of Raltegravir - The present invention provides novel salts of raltegravir, viz., meglumine salt, erbumine salt, ammonium salt, tris salt and L-arginine salt of raltegravir and processes for their preparation. | 06-05-2014 |
| 20140187778 | PEST CONTROL COMPOSITION - Disclosed is a pest control composition having an excellent controlling effect on pests, which comprises etoxazole and fenazaquin. | 07-03-2014 |
| 20150045554 | SYNTHESIS OF RALTEGRAVIR - The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V). | 02-12-2015 |
| 20150099883 | ARYLOXYUREA COMPOUND AND PEST CONTROL AGENT - The present invention provides an aryloxyurea compound or salt thereof, and a pest control agent including the aryloxyurea compound or salt thereof as an active ingredient. The aryloxyurea compound has a superior acaricidal and/or insecticidal activity, superior safety, and can be synthesized advantageously and industrially. The compound of the present invention includes aryloxyurea compounds represented by the following formula or salts thereof: | 04-09-2015 |
| 20150353526 | TETRAHYDROPHENANTHRIDINONES AND TETRAHYDROCYCLOPENTAQUINOLINONES AS PARP AND TUBULIN POLYMERIZATION INHIBITORS - The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) | 12-10-2015 |
| 20160024020 | INTERMEDIATES TO PREPARE HERBICIDAL PYRIMIDONE DERIVATIVES - Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, | 01-28-2016 |
| 20160137611 | PREPARATION METHOD FOR ACRYLATE COMPOUND - The present invention relates to a method for preparing an acrylate compound. The acrylate compound has a structure as shown in formula (I). The method includes: subjecting a compound with a structure of formula (II) or a mixture of compounds with structures of formula (I) and formula (II), and a catalyst to a contact reaction in the absence of an anhydride, and removing the resulting methanol by pressure reduced distillation during the contact reaction process. In the formulas (I) and (II), R is selected from one of: an alkoxy with a carbon number of 1-5, a substituent-containing phenoxyl with a carbon number of 6-20, a substituent-containing heteroaryloxy with a carbon number of 4-20, a substituent-containing heteroaryloxymethyl with a carbon number of 4-20, a substituent-containing phenoxymethyl with a carbon number of 5-20, and a substituent-containing alkyl with a carbon number of 2-20. According to the method for preparing an acrylate compound provided in the invention, the conversion rate and selectivity of the reaction can be substantially improved. | 05-19-2016 |
| 20160137612 | PROCESS FOR PREPARING 4,6-BIS (ARYLOXY) PYRIMIDINE DERIVATIVES - Process for preparing 4,6-bis(aryloxy)pyrimidine derivatives A process is provided for preparing 4,6-bis(aryloxy)pyrimidine derivatives. The process is conducted in water as reaction medium and catalyzed by one or more tertiary-amine catalyst(s). It has been found that a water based reaction substantially free of organic solvents can be carried out providing excellent yields by the addition of one or more tertiary-amine catalysts to the reaction medium. This provides a clean reaction and produces the desired product in high yields. | 05-19-2016 |
| 20160145215 | PROCESS FOR PREPARING A PYRIMIDINE INTERMEDIATE - The present invention relates to a process for preparing a pyrimidine intermediate, namely the compound of formula I-2 or a salt thereof. Said compound of formula I-2 or its salt can be used to prepare macitentan. Macitentan (chemical names: N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-propylsulfamide or N-[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]-N′-propylsulfuric diamide) is an endothelin receptor antagonist that has notably been approved by the US Food and Drug Administration and the European Commission for the treatment of pulmonary arterial hypertension. It has been first disclosed in WO 02/053557. The last step of one of the potential preparation routes described in WO 02/053557, called “Possibility A” and “Possibility B”, can be summarised as shown in Scheme A1 hereafter. | 05-26-2016 |
| 20160185766 | Novel Salts of Raltegravir - Provided herein are novel salts of raltegravir, viz., meglumine salt, erbumine salt, ammonium salt, tris salt and L-arginine salt of raltegravir and processes for their preparation. | 06-30-2016 |
| 20160194333 | CRYSTAL OF 6,7-UNSATURATED-7-CARBAMOYL MORPHINAN DERIVATIVE AND METHOD FOR PRODUCING THE SAME | 07-07-2016 |
| 20160200687 | Methods for Preparing Azoxystrobin and Intermediate Thereof | 07-14-2016 |
| 20170233369 | METALLOENZYME INHIBITOR COMPOUNDS AS FUNGICIDES | 08-17-2017 |
| 544320000 | Nitrogen attached directly at 2-position by nonionic bonding | 15 |
| 20140235858 | NEUROPROTECTIVE MULTIFUNCTIONAL ANTIOXIDANTS AND THEIR MONOFUNCTIONAL ANALOGS - The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: | 08-21-2014 |
| 544321000 | Carbocyclic ring containing | 14 |
| 20090062540 | METHODS OF PREPARING 4-PHENYL-6-(2,2,2-TRIFLUORO-1-PHENYLETHOXY)PYRIMIDINE-BASED COMPOUNDS - Methods useful for preparing compounds of formula I: | 03-05-2009 |
| 20090118505 | PROCESS FOR THE PREPARATION OF SUBSTITUTED PHENYLALANINES - Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g., of Formula I) are disclosed: | 05-07-2009 |
| 20100121060 | HIV INHIBITING 2-(4-CYANOPHENYL)-6-HYDROXYLAMINOPYRIMIDINES - HIV replication inhibitors of formula | 05-13-2010 |
| 20100234598 | PROCESS FOR THE PREPARATION OF IMATINIB AND INTERMEDIATES THEREOF - It is the object of the present invention a process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl- | 09-16-2010 |
| 20110124865 | PROCESS FOR THE PREPARATION OF SUBSTITUTED PHENYLALANINES - Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds are disclosed. | 05-26-2011 |
| 20110130564 | COMPOUNDS USEFUL IN THE PREPARATION OF TRYPTOPHAN HYDRROXYLASE INHIBITORS - Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g., of Formula I) are disclosed: | 06-02-2011 |
| 20110196156 | PROCESS FOR SYNTHESIS OF DIARYLPYRIMIDINE NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR - A method for synthesis of diarylpyrimidine non-nucleoside reverse transcriptase inhibitor such as etravirine is provided Typically, etravirine is synthesized by the steps of a Condensing 2,4,6-trichlorpyrimidine with 3,5-dimethyl-4-hydroxybenzonitrile to obtain compound (V), b Condensing compound (V) with 4-aminobenzonitrile to obtain compound (VI), c Ammonolysis of compound (VI) to get compound (IV), d Halogenation of compound (IV) to get etravirine. | 08-11-2011 |
| 20120083606 | PROCESS FOR PREPARING 4-[(1,6-DIHYDRO-6-OXO-2-PYRIMIDINYL)AMINO]BENZONITRILE - This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure. | 04-05-2012 |
| 20130116433 | PROCESS FOR THE PRODUCTION OF ETRAVIRINE - A novel process for the preparation of Etravirine comprises the condensing of ethyl cyanoacetate with N-cyanophenylguanidine to obtain an —OH compound of formula (II), which is further converted to a leaving group of formula (III). The compound of formula (III) is optionally protected and brominated to yield compound of formula (IV). The condensation of formula (IV) with 3,5-dimethyl-4-hydroxybenzonitrile yields a compound of formula (VI), and an optional deprotection of the compound of formula (VI) results in Etravirine. | 05-09-2013 |
| 20130123498 | PROCESS FOR THE PREPARATION OF ETRAVIRINE AND INTERMEDIATES IN THE SYNTHESIS THEREOF - The present invention includes compounds of Formula 1 of the following structure: | 05-16-2013 |
| 20130245261 | PROCESS FOR PREPARING PAN-CDK INHIBITORS OF THE FORMULA (I), AND INTERMEDIATES IN THE PREPARATION - The invention relates to a novel process for the preparation of pan-CDK inhibitors of the formula (I), and intermediates of the preparation. | 09-19-2013 |
| 20140213787 | REGIOSELECTIVE PREPARATION OF 2-AMINO-5-TRIFLUOROMETHYLPYRIMIDINE DERIVATIVES - The present invention relates to a method of making 2,4-differentiated 5-trifluoromethylpyrimidines, which are useful as intermediates in the manufacture of active pharmaceutical substances. | 07-31-2014 |
| 20150336900 | Process for the Synthesis of Etravirine and Its Intermediates - The invention discloses the synthesis of Etravirine via intermediate 4-((4-amino-5-bromo-6-chloropyrimidin-2-yl) amino)benzonitrile and process for the preparation of Etravirine of the formula-I. | 11-26-2015 |
| 20160159749 | METHODS OF REGIOSELECTIVE SYNTHESIS OF 2,4-DISUBSTITUTED PYRIMIDINES - The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions. | 06-09-2016 |
