Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2004-04-28
2008-09-09
Dentz, Bernard (Department: 1625)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
active
07423162
ABSTRACT:
The invention relates to a process for the preparation of (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile from 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one, wherein X stands for a leaving group, by reacting 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one with a cyanide ion in water and by subsequent lowering of the pH to a pH between 0 and 5. (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable from (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile may suitably be used in the preparation of a pharmaceutical preparation, more in particular in the preparation of statins, more in particular in the preparation of Atorvastatine or a salt thereof, for instance its calcium salt. The invention also relates to (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable therefrom.
REFERENCES:
patent: 2005/0153407 (2005-07-01), Greenberg et al.
patent: WO 89/07598 (1989-08-01), None
patent: WO 02/06266 (2002-01-01), None
Kelvin L. Baumann et al; “The Convergent Synthesis of CI-981, an Optically Active, Highly Potent, Tissue Selective Inhibitor of HMG-CoA Reductase”; Tetrahedron Letters, vol. 33, No. 17, pp. 2283-2284; 1992.
Peter W.K. Woo et al; Atorvastatin, An HMG-COA Reductase Inhibitor and Effective Lipid-Regulating Agent—Part III1a,bSyntheses of [2H5]-,[13CB], and [13C7,15N] Atorvastatin and Their Application in Metabolic and Pharmacokinetic Studies; Journal of Labelled Compounds and Radiopharmaceuticals J. Labelled Cpd. Radiopharm. 42, 135-145; (1999).
Philip L. Brower et al; “The Synthesis of (4R-cis)-1,1-Dimethylethyl 6-cyanomethyl-2,2-dimethyl-1,3-dioxane-4-acetate, a Key Intermediate for the Preparation of CI-981, A Highly Potent, Tissue Selective Inhibitor of HMG-CoA Reductase”; Tetrahedron Letters, vol. 33, No. 17; pp. 2279-1182; 1992.
William A. Greenberg et al; “Developmento f an Efficient, Scalable, Aldolase-Catalyzed Process for Enantioselective Synthesis of Statin Intermediates”; PNAS, Apr. 20, 2004; vol. 101, No. 16, pp. 5788-5793.
Boesten Wilhelmus Hubertus Joseph
Mink Daniel
Sereinig Natascha
Wolberg Michael
Dentz Bernard
DSM IP Assets B.V.
LandOfFree
Process for the preparation of... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Process for the preparation of..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process for the preparation of... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3976200