C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 309/00 (2006.01) A61K 31/40 (2006.01) A61P 3/00 (2006.01) A61P 3/06 (2006.01)
Patent
CA 2524457
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.
L'invention concerne un procédé de préparation de (4-hydroxy-6-oxo-tétrahydro-pyran-2-yl)-acétonitrile à partir de méthyl-4-hydroxy-tétrahydro-pyran-2-one 6-X-substituée, où X représente un groupe partant, par réaction de méthyl-4-hydroxy-tétrahydro-pyran-2-one 6-X-substituée avec un ion cyanure dans de l'eau et par abaissement subséquent du pH à un pH compris entre 0 et 5. Le (4-hydroxy-6-oxo-tétrahydro-pyran-2-yl)-acétonitrile et d'autres composés pouvant être obtenus à partir du (4-hydroxy-6-oxo-tétrahydro-pyran-2-yl)-acétonitrile peuvent avantageusement être utilisés dans la préparation d'une composition pharmaceutique, et plus particulièrement dans la préparation de statines, et notamment d'atorvastatine ou d'un sel correspondant, tel que son sel calcique. L'invention concerne également un (4-hydroxy-6-oxo-tétrahydro-pyran-2-yl)-acétonitrile ainsi que d'autres composés pouvant être obtenus à partir de celui-ci.
Boesten Wilhelmus Hubertus Joseph
Mink Daniel
Sereinig Natascha
Wolberg Michael
Dsm Ip Assets B.v.
Fetherstonhaugh & Co.
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