A practical synthesis and the pharmacological potency of gem-diphosphono substituted pyrimidines for treatment of bone resorption

A series of substituted arylidenes was allowed to react with the Wittig-Horner reagent, tetraethyl- methylene-1,1-bisphosphonate to give the corresponding N-containing bisphosphonates (BPs). Acid hydrolysis of one of the BPs gave the corresponding bisphosphonic acid. The in vivo anti- resorptive activities of the products in the rat adjuvant model are discussed in terms of structure- activity relationships (SAR).