PROCESS FOR PREPARING ASENAPINE AND SALTS OF INTERMEDIATES THEREOF

PROCESS FOR PREPARING ASENAPINE AND SALTS OF INTERMEDIATES THEREOF

A process for preparing substantially pure trans-5-chloro-2-methyl-2,3,3a42b4etrahydro-lH-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole (Asenapine) of formula (I) is provided. The salts of intermediates useful for preparing Asenapine of formula (I) i.e. 5-nitro-2-methyl-2,3,3a,12b-tetrahydro-lH-dibenz [2,3:6...

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Bibliographische Detailangaben
Hauptverfasser: PATEL, SAMIR, PARMAR, BHUPENDRA, JAYARAMAN, VENKAT, RAMAN, KONDEPATI, VENKAT, RAMAN, PATEL, RONAK, MISTRY, SAMIR, YADAV, GAURAV, PATIL, CHETAN, TAMBOLI, PARIMAL
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Zusammenfassung:A process for preparing substantially pure trans-5-chloro-2-methyl-2,3,3a42b4etrahydro-lH-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole (Asenapine) of formula (I) is provided. The salts of intermediates useful for preparing Asenapine of formula (I) i.e. 5-nitro-2-methyl-2,3,3a,12b-tetrahydro-lH-dibenz [2,3:6,7] oxepino [4,5-c]pyrrole of formula (VIII) and 5-amino-2-methyl-2,3,3a,12b-tetrahydro-lH-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole of formula (DC) are also provided. L'invention porte sur un procédé pour la préparation de trans-5-chloro-2-méthyl-2,3,3a,12b-tétrahydro-1H-dibenz[2,3:6,7]oxépino[4,5-c]pyrrole (asénapine) de formule (I) pratiquement pur. L'invention porte également sur les sels d'intermédiaires utiles pour la préparation d'asénapine de formule (I), c'est-à-dire du 5-nitro-2-méthyl-2,3,3a,12b-tétrahydro-1H-dibenz[2,3:6,7]oxépino[4,5-c]pyrrole de formule (VIII) et du 5-amino-2-méthyl-2,3,3a,12b-tétrahydro-1H-dibenz[2,3:6,7]oxépino[4,5-c]pyrrole de formule (DC).