Synthesis of novel (1-alkanoyloxy-4-alkanoylaminobutylidene)-1,1- bisphosphonic acid derivatives

Abstract

A novel strategy for the synthesis of (1-alkanoyloxy-4- alkanoylaminobutylidene)-1,1-bisphosphonic acid derivatives (1a-d) via (1-hydroxy-4-alkanoylaminobutylidene)-1,1-bisphosphonic acid derivatives (2a-d), starting from alendronate has been developed with reasonable 51-77% overall yields. Intermediate products, (1-hydroxy-4-alkanoylaminobutylidene)-1,1- bisphosphonic acid derivatives (2a-d), were prepared in water with reasonable to high yields (52-94%). © 2006Turhanen and Vepsäläinen; licensee Beilstein-Institut.