Journal
LETTERS IN DRUG DESIGN & DISCOVERY
Volume 15, Issue 7, Pages 713-720Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1570180814666171027160324
Keywords
Ibandronate; N-methyl-N-pentyl-beta-alanine; P-reagents; sulfolane; ionic liquid additive; osteoporosis
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Funding
- Gedeon Richter Plc
- Hungarian Research Development and Innovation Fund [K119202]
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Background: Ibandronate is a prominent representative of alpha-hydroxy-methylenebisphosphonic acid (dronic acid) derivatives applied in the treatment of bone diseases. Methods: Ibandronate was synthesized from N-methyl-N-pentyl-beta-alanine using phosphorus trichloride and phosphorous acid in different ratios, applying sulfolane as the solvent (1.), or under solvent-free conditions (2.), or in ionic liquids as additives (3.). Results: In the first two cases (1. and 2.), using phosphorus trichloride and phosphorous acid in molar ratios of 2:4 and 3:4, pure ibandronate was obtained in yields of 72- 83%. In the presence of 10% of [bmim][BF4] as an additive (3.), a better yield of 82/90% was obtained applying ratios of 2:2 and 3:2 of the P-reagents assuming less of the phosphorous acid. Conclusion: The new methods developed mean record outcomes in respect of the valuable drug, ibandronate.
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