PROCESS FOR PREPARATION OF NEBIVOLOL AND IT'S SALTS

The present invention discloses a new process for preparation of Nebivolol or it's pharmaceutically acceptable salt. More particularly, the invention discloses an improved economical process for the preparation of intermediate, 6-fluoro-3,4- dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula -...

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Bibliographische Detailangaben
Hauptverfasser:	MORE, Kishor Ramdas, BUCHI, Reddy Reguri, PATIL, Yuvaraj, CHAVAN, Navanath Maruti, CHOUDHARI, Shailesh Mallikarjun, CHIDURALA, Rajashekhar, SADAKAL, Jeevan Bharat, GAWADE, Sanjay Pandurang, MALEKAR, Sachin, KUMAR, Ashok
Format:	Patent
Sprache:	eng ; fre
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Beschreibung
Zusammenfassung:	The present invention discloses a new process for preparation of Nebivolol or it's pharmaceutically acceptable salt. More particularly, the invention discloses an improved economical process for the preparation of intermediate, 6-fluoro-3,4- dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula - II, converting the 6- fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula - II into mixture of [R(S)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran and [R(R)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran of Formula-V and separation of diastereomers of (R)-6-Fluoro-3,4-dihydro-2-((S)-oxiran-2-yl)- 2H-benzopran by forming azeotrope. La présente invention concerne un nouveau procédé de préparation de nébivolol ou de son sel pharmaceutiquement acceptable. Plus particulièrement, l'invention se rapporte à un procédé économique amélioré pour la préparation de l'intermédiaire 6-fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxaldéhyde de Formule II, consistant à convertir le 6-fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxaldéhyde de Formule II en un mélange de [R(S)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyrane et [R(R)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran de Formule V, et à séparer les diastéréomères de (R)-6-fluoro-3,4-dihydro-2-((S)-oxiran-2-yl)-2H-benzopyran par formation d'un azéotrope.