Processes for preparing ezetimibe and intermediate compounds...

Details Processes for preparing ezetimibe and intermediate compounds... Processes for preparing ezetimibe and intermediate compounds...

C - Chemistry, Metallurgy

07

D

C07D 205/08 (2006.01)

Patent

CA 2647902

The invention relates, in general, to an improved process for converting compounds of Formula II (below) to compounds of Formula III (below), which are key intermediates for the synthesis of ezetimibe, or to ezetimibe itself, wherein in Formulas II and III, R represents hydrogen, alkyl, or a hydroxyl protecting group (e.g., benzyl group, a substituted benzyl group, or a silyl group). The invention further includes the use of the described process and the use of compounds of Formula III made by the described process for the preparation of ezetimibe.

La présente invention concerne de façon générale un procédé amélioré de conversion de composés de Formule (II) (ci-dessous) en composés de Formule (III) (ci-dessous), qui sont des intermédiaires clés dans la synthèse de l'ézétimibe, ou l'ézétimibe lui-même, où dans les Formules (II) et (III), R représente un atome d'hydrogène ou un groupement alkyle ou protecteur de groupement hydroxy (par exemple benzyle, benzyle substitué ou silyle). La présente invention concerne également l'emploi du procédé décrit et l'emploi des composés de Formule (III) fabriqués à l'aide du procédé décrit dans la synthèse de l'ézétimibe.

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