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US 2011/0237808 A1Published application
Method for preparing nebivolol
AssigneeZach System S.P.A.
InventorsYvon Derrien, Eric Chenard, Alain Burgos
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Abstract
The present invention relates to a process for the preparation of nebivolol and, more particularly, to an improved process of synthesizing an alpha-haloketone of formula a key intermediate in the preparation of nebivolol.
Claims17
A process for preparing a compound of formula
- wherein X is a halogen atom,
- which comprises reacting with a halomethyllithium derivative a compound of formula
- wherein R is a (C1-C6)-alkyl group.
A process for preparing a compound of formula
- which comprises a step of converting a compound of formula VI
- wherein R is a (C1-C6)-alkyl group
- into a compound of formula I
- wherein X is a halogen atom by reacting said compound of formula VI with a halomethyllithium derivative.
1 more element
A process for preparing a compound of formula
- which comprises
- a) reacting with a halomethyllithium derivative a compound of formula
- wherein R is a (C1-C6)-alkyl group to give a reaction mixture;
- b) in situ reducing said reaction mixture;
- and
- c) cyclizing in the presence of a base.
3 more elements
A compound of formula
- wherein X is a halogen atom and R is a (C1-C6)-alkyl group.
A process for the preparation of nebivolol which comprises a step of converting a compound of formula VI
- wherein R is a (C1-C6)-alkyl group into a compound of formula I
- wherein X is a halogen atom by reacting said compound of formula VI with a halomethyllithium derivative.
A process for the preparation of nebivolol which comprises a one-pot conversion of a compound of formula VI
- wherein R is a (C1-C6)-alkyl group into a compound of formula VII.
- said one-pot conversion comprising:
- a) reacting said compound of formula VI with a halomethyllithium derivative to give a reaction mixture;
- b) in situ reducing said reaction mixture;
- and
- c) cyclizing the resulting product in the presence of a base.
3 more elements
Dependencies are inferred from the claim text.