abstract |
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. |