Process for making bisphosphonic acids using diluents other...

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

Reexamination Certificate

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C546S022000

Reexamination Certificate

active

07038083

ABSTRACT:
Provided is a novel method of making bisphosphonic acids, e.g. risedronic acid, including the step of combining a carboxylic acid, phoshorous acid, and a halophosphorous compound in the presence of a diluent that is an aromatic hydrocarbon or a silicone fluid. When the diluent is an aromatic hydrocarbon, a inert support or ortho-phosphoric acid codiluent is advantageously included.

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Kieczykowski et al., “Preparation of (4-Amino-1-Hydroxybutylidene) bisphosphonic Acid Sodium Salt MD-217 (Alendronate Sodium). An Improved Procedure for the Preparation of 1-Hydroxy-1, 1-bisphosphonic Acids”,J. Org. Chem,60 (25)8310, 8311 (1995).
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