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Rational Synthesis of Ibandronate and Alendronate

[ Vol. 10 , Issue. 4 ]


Gyorgy Keglevich, Alajos Grun, Rita Kovacs, Sandor Garadnay and Istvan Greiner   Pages 640 - 644 ( 5 )


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).


Ibandronate, Alendronate, Synthesis, Optimization, Intermediate.


Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest, Hungary.

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