| abstract |
A novel process for the preparation of alendronic acid is revealed. The method comprises the steps of: reacting a compound of the formula (I) (see formula) with H3PO3, wherein R is an imido group and RI is selected from the group consisting of chlorine, bromine, iodine, fluoro, hydroxy, amino , -OR2 or -OC (O) R2, wherein R2 is C1-C12 alkyl, C1-C12 cycloalkyl, or C1-C12 aryl; and then react the product of the first step with a deprotecting agent. Then alendronic acid is recovered. The method is safe, efficient and suitable for large-scale use. |