Synthesis of Pharmacologically Active 2-Substituted-1,3-Diphosphonates

Abstract

A new series of diphosphonates (I) was synthesized and investigated for their pharmacological activity. 2-Substituted-1,3-propylidene diphosphonates (I) were prepared by reaction of sodium dialkyl phosphite or trialkyl phosphite with ditosylates of 2-substituted-1,3-propanediol or 2-substituted-1,3-dibromopropane. Pharmacological screenings of these 1,3-propylidenediphosphonates have shown that these compounds have potent cardiovascular activity and are potentially useful in the treatment of hypertension.