75439-01-9Relevant articles and documents
MOXONIDINE ANALOGS, PREPARATION PROCESSES AND USES THEREFOR
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Page/Page column 12, (2008/12/06)
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.
Improved process for producing moxonidine
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Page/Page column 7, (2008/06/13)
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.