Process for preparation of 4,5-epoxymorphinan-6-oxyglucuronides

Details Process for preparation of 4,5-epoxymorphinan-6-oxyglucuronides Process for preparation of 4,5-epoxymorphinan-6-oxyglucuronides

C - Chemistry, Metallurgy

07

H

C07H 17/00 (2006.01) C07H 17/08 (2006.01)

Patent

CA 2331866

Conjugation of 4,5-Epoxymorphinan-6-ols with Bromoglucuronides in the presence of Zinc containing compounds as activator under conditions capable of forming 4,5-Epoxymorphinan-6-oxyglucuronides is disclosed. This novel approach provides an efficient method for preparation of both anomers of 4,5- Epoxymorphinan-6-oxyglucuronides. The deprotected end products are useful as analgesic agents.

On décrit un procédé conjuguant des 4,5 époxymorphinan-6-oles et des bromoglucuronides en présence de composés à base de zinc utilisés comme activateurs, dans des conditions permettant la formation de 4,5 époxymorphinan-6-oxyglucuronides. Cette nouvelle approche fournit une méthode efficace de préparation des deux anomères de 4,5 époxymorphinan-6-oxyglucuronides. Les produits finis déprotégés ainsi obtenus s'utilisent comme analgésiques.

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