Rational Synthesis of Ibandronate and Alendronate

Title:Rational Synthesis of Ibandronate and Alendronate

Volume: 10 Issue: 4

Author(s): Gyorgy Keglevich, Alajos Grun, Rita Kovacs, Sandor Garadnay and Istvan Greiner

Affiliation:

Keywords: Ibandronate, Alendronate, Synthesis, Optimization, Intermediate.

Abstract: Ibandronate and Alendronate/Alendronic acid were prepared by the reaction of the corresponding amino acids (N-methyl-Npentylalanine and γ-aminobutyric acid) with 3.2 equivalents of phosphorus trichloride, in the absence of any phosphorous acid, in methanesulfonic acid at 75 °C for 12 h followed by hydrolysis, pH adjustment and purification. The first intermediate of the reaction sequence is the corresponding chloride (>N(CH2)nC(O)Cl) or mixed ester (>N(CH2)nC(O)OS(O)2Me).

Cite this article as:

Keglevich Gyorgy, Grun Alajos, Kovacs Rita, Garadnay Sandor and Greiner Istvan, Rational Synthesis of Ibandronate and Alendronate, Current Organic Synthesis 2013; 10 (4) . https://dx.doi.org/10.2174/1570179411310040007