Processes for preparing intermediate compounds useful for...

C - Chemistry – Metallurgy – 07 – D

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C07D 205/08 (2006.01) C07D 263/24 (2006.01)

Patent

CA 2634648

The invention relates, in general, to an improved process for the preparation of the compounds (3R,4S)-4-(4-(benzyloxy)phenyl)-l-(4-fluorophenyl)-3-[3-(4- fluorophenyl)-3- oxopropyl]azetidin-2-one and (3R,4S)-l-(4-fluorophenyl)-3-[3- (4-fluorophenyl)-3-oxopropyl]- 4-(4-hydroxyphenyl)-azetidin-2-one, which are key intermediates for the synthesis of ezetimibe, as well as the use of these intermediates for the preparation of ezetimibe.

L'invention concerne, d'une manière générale, un procédé amélioré pour la préparation des composés (3R,4S)-4-(4-(benzyloxy)phényl)-l-(4-fluorophényl)-3- [3-(4-fluorophényl)-3- oxopropyl]azétidin-2-one et (3R,4S)-l-(4-fluorophényl)-3-[3-(4-fluorophényl)-3-oxopropyl]- 4-(4-hydroxyphényl)-azétidin-2-one, qui sont les intermédiaires clés de la synthèse de l'ézétimide, ainsi que l'utilisation de ces intermédiaires dans la préparation de l'ézétimide.

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