- SYNTHESIS OF SUBSTITUTED AMINOPYRIMIDINES
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The present invention relates to a novel process for the manufacture of certain substituted aminopyrimidines having Formula (I) or a tautomer or salt thereof, wherein R1 is selected from hydrogen, halogen, C1-4alkoxy, C1-4alklthio, C1-4alkyl, C3-5cycloalkyl, for example R1 is halogen such as chloro; R2 is C1-4alkyl, for example methyl, ethyl, i-propyl, n-propyl or butyl (any isomer), such as methyl; and R3 is selected from hydrogen, C1-4alkoxy, C1-4alkylthio, C1-4alkyl, C3-5cycloalkyl, for example C1-4alkyl such as methyl, ethyl, i-propyl, n-propyl or butyl (any isomer), for example methyl; crystalline forms thereof as well as chemical intermediates suitable for use in performing the process.
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Page/Page column 17; 18
(2015/02/19)
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- Synthesis of substituted aminopyridines
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The present invention relates to a novel process for the manufacture of certain substituted aminopyridines having Formula (I) or a tautomer or salt thereof, wherein R1 is selected from hydrogen, halogen, C1-4alkoxy, C1-4alklthio, C1-4alkyl, C3-5cycloalkyl, for example R1 is halogen such as chloro; R2 is C1-4alkyl, for example methyl, ethyl, i-propyl, n-propyl or butyl (any isomer), such as methyl; and R3 is selected from hydrogen, C1-4alkoxy, C1-4alkylthio, C1-4alkyl, C3-5cycloalkyl, for example C1-4alkyl such as methyl, ethyl, i-propyl, n-propyl or butyl (any isomer), for example methyl; crystalline forms thereof as well as chemical intermediates suitable for use in performing the process.
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Paragraph 0041
(2015/02/25)
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- PROCESS FOR THE PRODUCTION OF MOXONIDINE
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4,6-dichloro-2-methyl-5-(1-acyl-2-imidazolin-2-yl)-aminopyrimidine is reacted with methanol in the presence of a non-ionic organic base, and moxonidine is obtained directly from the reaction mixture.
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Paragraph 0057-0058
(2014/08/19)
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- Method by means of phase transfer catalysis
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The invention relates to a method for preparing a compound having the formula (I): where R is an aliphatic and/or aromatic radical, wherein 4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine and an alcohol are caused to react in the presence of a phase transfer catalyst.
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Paragraph 0080
(2014/06/24)
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- Process for the preparation of moxonidine
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The present invention provides an improved process for the preparation of 4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)aminopyrimidine. The present invention also provides an improved process for the preparation of moxonidine. The present invention further provides a process for the purification of moxonidine.
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Paragraph 0037
(2013/05/09)
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- MOXONIDINE ANALOGS, PREPARATION PROCESSES AND USES THEREFOR
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The present invention provides derivatives of moxonidine, 1-[l-[(4,6-dichloro-2-methyl-6-5-pyrimidinyl)imino]ethyl]-2-imidazolidinone of formula (V) and l-[l-[(4-chloro-2-methyl-6-methoxy-5-pyrimidinyl)imino]ethyl]-2-imidazolidinone of formula (VI), which can be used for testing the purity or monitoring the production of moxonidine, and process for preparing the derivatives. Also provided is an improved process for preparing 4,6- dichloro-2-methyl-5-(l-acetyl-2-imidazolin-2-yl)-aminopyrimidine (DMAIA) and a method of utilizing the process to produce moxonidine.
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Page/Page column 12
(2008/12/06)
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- Polymorphs of moxonidine and processes for preparation therefor
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Three crystalline forms of Moxonidine designated as Moxonidine form I, form II and form III and processes for their preparation are disclosed.
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Page/Page column 7
(2008/06/13)
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- Novel purification process of moxonidine
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The present invention provides a novel purification process of Moxonidine avoiding nitromethane and using instead class 3 solvents or selected class 2 solvents for preparing highly pure Moxonidine, e.g, the crystalline Moxonidine form I.
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Page/Page column 7
(2008/06/13)
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- The use of moxonidine salts for purification of moxonidine
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The present invention provides crystalline Moxonidine salts e.g., mono-Moxonidine oxalate and mono-Moxonidine formate. Also provided by the present invention is a novel purification process of Moxonidine using these crystalline Moxonidine salts. By precipitating a Moxonidine salt from the reaction mixture and reacting it with a base, highly pure crystalline Moxonidine base is obtained in high yield.
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Page/Page column 9
(2008/06/13)
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- Improved process for producing moxonidine
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The present invention provides improved process for production of highly pure Moxonidine comprising reacting the starting material 6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine (DMAIA) with different bases (e.g., sodium hydroxide or potassium hydroxide), thus avoiding the use of sodium methoxide while carrying out the reaction at milder conditions. While using sodium methoxide, is not needed to use methanol as solvent and a more friendly class 3 solvent (e.g., DMSO) is used instead. The reaction may be carried out at ambient temperature and it is not necessary to use two-fold excess of the base as about 1.0-1.1 molar excess of sodium methoxide in relation to DMAIA is sufficient.
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Page/Page column 6
(2008/06/13)
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- USE OF SUBSTITUTED 2 PHENYLBENZIMIDAZOLES AS MEDICAMENTS
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The present invention relates to the use of a substituted 2-phenylbenzimidazole of formula I wherein R1, R2, R3, R 4, R5 and m have the meanings given in the claims, for the preparation of a medicament for the treatment or prevention of diseases involving glucagon receptors, as well as new compounds of formula I wherein R1 is a group of formula
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- Feed additive for improving growth in agricultural animals
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By using α-mimetics, particularly compounds of general formulae I to III and the compounds listed in Table I, as feed additives in fattening animals, it has surprisingly been possible to improve the daily weight gain, the utilisation of fodder and the ratio of muscle to fat in favor of the proportion of muscle and protein.
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- Substituted aminopyrimidines
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The present invention is directed to certain aminopyrimidines of the general formula STR1 wherein R1, R2, and R3 are hydrogen, halogen, alkoxy, alkylthio, or alkyl having 1 to 4 carbon atoms, or cycloalkyl having 3 to 5 carbon atoms and R4 is hydrogen or an aliphatic or aromatic acyl group, as well as physiologically compatible acid addition salts thereof. Compounds of the present invention are useful as blood pressure lowering agents and in the treatment of glaucoma.
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