Epimerisation of allylic alcohols

C - Chemistry – Metallurgy – 07 – C

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C07C 401/00 (2006.01) A61K 31/59 (2006.01)

Patent

CA 2572607

The present invention relates to processes for epimerising alcohols of compounds having a hydroxyl substituent on an asymmetric allylic carbon, such as compounds useful for the synthesis of vitamin D analogues where the epimeric hydroxyl substituents is at the 24 position. The invention further relates to methods of producing intermediates useful for the synthesis of calcipotriol (I) or calcipotriol monohydrate (I-hydrate) by said epimerization processes (see formula I), (see formula I-hydrate)

L'invention concerne des procédés pour épimériser des alcools de composés présentant un substituant hydroxyle sur un carbone allylique asymétrique. De tels composés sont utiles pour la synthèse d'analogues de la vitamine D dans lesquels le substituant hydroxyle épimérique est en position 24. L'invention concerne également des méthodes de production d'intermédiaires utiles pour la synthèse de calcipotriol par des procédés d'épimérisation.

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