PROCESS FOR THE PREPARATION OF FLIBANSERIN INVOLVING NOVEL INTERMEDIATES
The present invention related to process for the preparation of flibanserin involving novel intermediates. 1,3-dihydro-1-(2-bromoethyl)- 3-isopropenyl-2H-benzimidazol-2-one reacts with diethanolamine and converting the obtained dihydroxy compound to 1,3-dihydro- 1-[2-[N-[bis-(2-chloroethyl)amino]eth...
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Zusammenfassung: | The present invention related to process for the preparation of flibanserin involving novel intermediates. 1,3-dihydro-1-(2-bromoethyl)- 3-isopropenyl-2H-benzimidazol-2-one reacts with diethanolamine and converting the obtained dihydroxy compound to 1,3-dihydro- 1-[2-[N-[bis-(2-chloroethyl)amino]ethyl]-3-isopropenyl-2H-benzimidazol-2-one followed by depotection to obtain 1,3-dihydro- 1-[2-[N-bis-(2-chloroethyl)amino]ethyl]-1,2-H-benzimidazol-2-one. This on condensing with m-trifluoromethyl aniline gives flibanserin hydrochloride.
Cette invention concerne un procédé de préparation de la flibansérine impliquant de nouveaux intermédiaires. Le composé 1,3-dihydro-1-(2-bromoéthyl)-3-isopropényl-2H-benzimidazol-2-one réagit avec la diéthanolamine et convertit le composé dihydroxy obtenu en 1,3-dihydro-1-[2-[N-[bis-(2-chloroéthyl)amino]éthyl]-3-isopropényl-2H-benzimidazol-2-one, pour obtenir au final 1,3-dihydro-1-[2-[N-bis-(2-chloroéthyl)amino]éthyl]-1,2-H-benzimidazol-2-one. La condensation de ce composé avec la m-trifluorométhyl aniline permet d'obtenir du chlorhydrate de flibansérine. |
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