TREA

Process for the preparation of risedronate sodium hemi-pentahydrate

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  • Patent Application
  • 20070173484
  • Publication Number
    20070173484
  • Date Filed
    January 16, 2007
    17 years ago
  • Date Published
    July 26, 2007
    17 years ago
Information
Abstract
The present invention relates to an improved process for the selective crystallization of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid sodium in pure hemi-pentahydrate form of Formula (I), by first converting 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid into organic amine salt and then by replacing it with sodium salt.
Description
Claims
  • 1. An improved process for the selective preparation of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid sodium hemi-pentahydrate form of Formula (I),
  • 2. The process according to claim 1, wherein the base used is selected from sodium methoxide, sodium ethanoate, sodium propanoate, sodium butanoate, sodium pentanoate, sodium-2-ethylhexanoate, sodium lactate, sodium acetate or mixtures thereof.
  • 3. The process according to claim 2, wherein the base is preferably sodium 2-ethylhexanoate.
  • 4. The process according to claim 1, wherein the solvent used is selected from alcohol, esters, ethers, ketones, amides, nitriles or mixtures thereof, preferably alcohol.
  • 5. The process according to claim 4, wherein the alcohol used is selected from methanol, ethanol, isopropanol.
  • 6. The process according to claim 5, wherein the alcohol is methanol.
  • 7. A process for the preparation of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid of Formula (III)
  • 8. The process according to claim 7, wherein the organic amine base is selected from primary amine, secondary amine, tertiary amine.
  • 9. The process according to claim 8, wherein the organic amine base is tertiary amine.
  • 10. The process according to claim 9, wherein the tertiary amine is selected from triethylamine, tributylamine, ethyldiisopropylamine, N-methylmorpholine, triisooctylamine, pyridine, 2,6-lutidine, quinoline, preferably triethylamine.
  • 11. An improved process for the selective preparation of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid sodium in hemi-pentahydrate form of Formula (I),
  • 12. The process according to claim 11, wherein the organic amine base is selected from primary amine, secondary amine, tertiary amine.
  • 13. The process according to claim 12, wherein the organic amine base is tertiary amine.
  • 14. The process according to claim 13, wherein the tertiary amine is selected from triethylamine, tributylamine, ethyldiisopropylamine, N-methylmorpholine, triisooctylamine, pyridine, 2,6-lutidine, quinoline, preferably triethylamine.
  • 15. The process according to claim 11, wherein the base used in step (b) is selected from sodium methoxide, sodium ethanoate, sodium propanoate, sodium butanoate, sodium pentanoate, sodium-2-ethylhexanoate, sodium lactate, sodium acetate or mixtures thereof.
  • 16. The process according to claim 15, wherein the base is preferably sodium 2-ethylhexanoate.
  • 17. The process according to claim 11, wherein the solvent used in step (b) is selected from alcohol, esters, ethers, ketones, amides, nitrites or mixtures thereof, preferably alcohol.
  • 18. The process according to claim 17, wherein the alcohol used is selected from methanol, ethanol, isopropanol.
  • 19. The process according to claim 18, wherein the alcohol is methanol.
Priority Claims (1)
Number Date Country Kind
94/CHE/2006 Jan 2006 IN national