Process for manufacturing bisphosphonic acids

A technology of diphosphonic acid and phosphoric acid, applied in chemical instruments and methods, compounds of Group 5/15 elements of the periodic table, organic chemistry, etc., can solve problems such as unsatisfactory yield and purity
CN101443341AInactive Publication Date: 2009-05-27ALBEMARLE CORP

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ALBEMARLE CORP
Publication Date
2009-05-27
Estimated Expiration
Not applicable · inactive patent

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Abstract

A manufacturing process for the preparation of bisphosphonic acids and in particular zoledronic acid is provided, wherein diglyme, monoglyme, or a mixture thereof, is utilized to produce a homogenous, water soluble, solid reaction mass that upon cooling, dissolving in water and stripping results in a high purity product and comparatively good yield, wherein R1 is selected from the group composed as follows.
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Description

Background of the invention

[0001] The present invention relates to the preparation of bisphosphonic acids and pharmacologically active salts thereof, in particular 1-hydroxy-2-(imidazol-1-yl)ethylidene-1,1-diphosphine commonly known as zoledronic acid Improved industrial process for acids. The bisphosphonates described herein are suitable for use in the treatment of diseases of the skeletal system and in conditions when bone formation and / or calcium metabolism have been disturbed, eg in the treatment of bone displacements.

[0002] The bisphosphonic acids described herein have the following structures:

[0003]

[0004] In the formula, M1, M2, M3 and M4 are selected from hydrogen and monovalent cations, and R1 is selected from one of the following:

[0005] CH 3 etidronic acid

[0006] Zoledronic acid

[0007] risedronic acid

[0008] minodronic aci...

Claims

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