Process for preparing nebivolol
AssigneeZach System S.P.A.
InventorsElio Ullucci, Paolo Maragni, Livius Cotarca, Johnny Foletto
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Abstract
The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved process for synthesizing enantiomerically enriched 6-fluoro chroman alcohol or epoxide derivatives of formula, wherein R and X is defined in the description; as useful intermediates in the preparation of Nebivolol.
Claims28
A process for the separation of racemic terminal epoxide of formula
- wherein R is a group of formula
- to give an enantiomerically enriched substituted alcohol of formula
- wherein X is, hydroxy or amino group;
- and, respectively, an enantiomerically enriched epoxide of formula
- which comprises a hydrolytic or aminolytic kinetic resolution carried out in the presence of a non-racemic transition metal-ligand catalyst complex.
A process for the separation of racemic terminal epoxide of formula
- to give an enantiomerically enriched substituted alcohol of formula
- wherein X is defined above;
- and, respectively, an enantiomerically enriched epoxide of formula
- which comprises a hydrolytic or aminolytic kinetic resolution carried out in the presence of a non-racemic transition metal-ligand catalyst complex.
A compound of formula:
- [(R)-2-((R)-6-fluoro-chroman-2-yl)-2-hydroxy-ethyl]-carbamic acid benzyl ester;
- [(S)-2-((S)-6-fluoro-chroman-2-yl)-2-hydroxy-ethyl]-carbamic acid benzyl ester;
- [(R)-2-((S)-6-fluoro-chroman-2-yl)-2-hydroxy-ethyl]-carbamic acid benzyl ester;
- [(S)-2-((R)-6-fluoro-chroman-2-yl)-2-hydroxy-ethyl]-carbamic acid benzyl ester.
Use of (S,S)-Co (salen) or (R,R)-Co (salen) catalyst complex in the separation of racemic terminal epoxide of formula I.
Use of (S,S)-Co (salen) or (R,R)-Co (salen) catalyst complex in the preparation of NBV.
Dependencies are inferred from the claim text.