[EN] PROCESS FOT THE PREPARATION OF (4-HYDROXY-6-OXO-TETRAHYDROPYRAN-2-YL) ACETONITRILE AND DERIVATIVES THEREOF<br/>[FR] PROCEDE DE PREPARATION DE (4-HYDROXY-6-OXO-TETRAHYDROPYRAN-2-YL)-ACETONITRILE ET DE DERIVES CORRESPONDANTS
申请人:DSM IP ASSETS BV
公开号:WO2004096788A1
公开(公告)日:2004-11-11
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.
该发明涉及一种从6-X-取代-甲基-4-羟基-四氢吡喃-2-酮制备(4-羟基-6-氧代-四氢吡喃-2-基)-乙腈的方法,其中X代表一个离去基团,通过在水中将6-X-取代-甲基-4-羟基-四氢吡喃-2-酮与氰离子反应,然后将pH降低至0至5之间的pH。从(4-羟基-6-氧代-四氢吡喃-2-基)-乙腈获得的化合物和其他化合物可适用于制备药物制剂,更具体地用于制备他汀类药物,更具体地用于制备阿托伐他汀或其盐,例如其钙盐。该发明还涉及(4-羟基-6-氧代-四氢吡喃-2-基)-乙腈和可从中获得的其他化合物。