Novel process for the preparation of bisphosphonic acids

C - Chemistry – Metallurgy – 07 – F

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C07F 9/38 (2006.01) C07F 9/58 (2006.01)

Patent

CA 2656053

The present invention relates to a process for the preparation of bisphosphonic acids and salts thereof, in particular monosodium salts thereof. The invention also relates to the conversion of the bisphosphonic acids to their sodium salts using an aqueous-organic solvent system. The present invention further relates to the conversion of variable hydrate forms of risedronic acid monosodium salt into a pharmaceutically acceptable hemipentahydrate form by crystallization using an aqueous-organic solvent system.

La présente invention concerne un procédé pour la préparation d'acides bisphosphoniques et de leurs sels, en particulier de leurs sels monosodiques. L'invention concerne également la conversion des acides bisphosphoniques en leurs sels de sodium à l'aide d'un système solvant aqueux-organique. La présente invention concerne en outre la conversion de diverses formes hydrates de sel monosodique d'acide risédronique en une forme hémipentahydrate pharmaceutiquement acceptable par cristallisation à l'aide d'un système solvant aqueux-organique.

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