3-alkyl-5-(4-alkyl-5-oxo-tetrahydrofutran-2-yl)...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 405/04 (2006.01) C07D 207/26 (2006.01) C07D 307/32 (2006.01) C07F 1/02 (2006.01)

Patent

CA 2625034

The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, or a salt thereof, and a compound of formula Vl or a salt thereof, wherein R3 and R4 as well as Act are as defined in the specification, and processes of manufacturing these. Additionally transformation of compounds (Vl) with metallo organic compounds (VII) give rise to the new compounds (VMI) which are direct precursors for the preparation of Aliskiren.

L'invention concerne un nouveau procédé, les étapes du nouveau procédé et de nouveaux intermédiaires utilisés dans la synthèse de composés actifs d'un point de vue pharmaceutique, en particulier des inhibiteurs de rénine, tels que l'aliskirène. L'invention concerne, entre autres, un procédé de fabrication d'un composé représenté par la formule II, ou un sel de celui-ci, et un composé représenté par la formule Vl ou un sel de celui-ci, R3 et R4 et Act étant tels que définis dans les spécifications, et des procédés de fabrication de ceux-ci. De plus, la transformation des composés (Vl) avec des composés métallo-organiques (VII) permet d'obtenir de nouveaux composés (VMI) constituant des précurseurs directs utilisés dans la préparation de l'aliskirène.

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