Process for preparing nebivolol

Details Process for preparing nebivolol Process for preparing nebivolol

2009-03-16

2011-12-27

Dentz, Bernard (Department: 1622)

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

active

08084629

ABSTRACT:
The present invention relates to a process for reducing a compound of formula (I) wherein X is halogen, a hydroxy group, an alkylsulfoniloxy group or an arylsulfonyloxy group; to give a compound of formula (II) as a diastereoisomerically pure compound of RS/SR configuration characterized in that said reduction is carried out by the use of (+)-B-chlorodiisopinocampheylborane or (−)-B-chlorodiisopinocampheylborane. The compounds of formula (II) are useful as intermediates for the preparation of Nebivolol.

REFERENCES:
patent: 1 803 715 (2007-07-01), None
patent: 2008/064826 (2008-06-01), None
Ramachandran, P.V. et al., “Efficient general synthesis of 1,2- and 1,3-diols in high enantiomeric excess via the intramolecular asymmetric reduction of the corresponding ketoalkyl diisopinocampheylborinate intermediates” Tetrahedron Letters, vol. 38., No. 5, 1997, pp. 761-764.
Srebnik, M. et al., “Chiral synthesis via organoboranes. 18. Selective reductions. 43. Diisopinocampheylchloroborane as an excellent chiral reducing reagent for the synthesis of halo alcohols of high enantiomeric purity. A highly enantioselective synthesis of both optical isomers of Tomoxetine, Fluoxetine, and Nisoxetine” J. Org. Chem., vol. 53., No. 13, 1988, pp. 2916-2920.
Cho, B.T. et al., “Facile Synthesis of Optically Active Styrene Oxide Derivatives by Asymmetric Reduction of Substituted 2-Sulfonyloxyacetophenomes with (−)-B-Chlorodiisopinocampheylborane” Bulletin of the Korean Chemical Society, vol. 22., No. 5, 2001, pp. 443-444.

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