Rational Synthesis of Ibandronate and Alendronate

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

Journal Name: Current Organic Synthesis

Volume 10 , Issue 4 , 2013

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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).

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

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Article Details

Year: 2013
Page: [640 - 644]
Pages: 5
DOI: 10.2174/1570179411310040007

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