Rational synthesis of Ibandronate and Alendronate

Keglevich, György and Grün, Alajos and Kovács, Rita and Garadnay, Sándor and Greiner, István (2013) Rational synthesis of Ibandronate and Alendronate. CURRENT ORGANIC CHEMISTRY, 10. pp. 640-644. ISSN 1385-2728

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Abstract

Ibandronate and Alendronate/Alendronic acid were prepared by the reaction of the corresponding amino acids (N-methyl-Npentylalanine and �-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).

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