Process for preparing nebivolol

Details Process for preparing nebivolol Process for preparing nebivolol

2011-08-16

2011-08-16

Dentz, Bernard (Department: 1622)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C549S213000, C549S453000

Reexamination Certificate

active

07999124

ABSTRACT:
The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.

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Chandrasekhar, et al., Enantioselective total synthesis of the antihypertensive agent (S,R,R,R)-nebivolol, Tetrahedron, 2000, 56:6339-6344.
Yu, et al., A Convenient Synthesis of 1-[6-Fluoro-(2S)-3H,4H-dihydro-2H-2-chromenyl]-. (1R)-1,2-ethanediol and 1-[6- Fluoro-(2R)-3H,4H-dihydro-2H-2-chromenyl]-. (1R)-1,2-ethanediol, Synlett, 2005, 9:1465-1467.
Johannes, et al., Zr-catalyzed kinetic resolution of allylic ethers and Mo-catalyzed chromene formation in synthesis. Enantioselective total synthesis of the antihypertensive agent (S,R,R,R)-nebivolol, J. Am. Chem. Soc., 1998, 120 (33):8340-8347.
Yang, et al., Synthesis and resolution research of (R)- and (S)-6-fluorochroman-2-carboxylic acids, Chinese Journal of Organic Chemistry, 2005, 25(2):201-203.

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