Process for preparing 3-alkeny-lidene-1, 1-bisphosphonates.

摘要

A process is provided for preparing a 3-alkenylidenel-l,l-bisphosphonate which is an intermediate for preparing an inhibitor of the enzyme squalene synthetase and therefore useful as an inhibitor of cholesterol biosynthesis, or which bisphosphonate itself is useful as an inhibitor of cholesterol biosynthesis. The process involves the palladium catalyzed coupling of an allylic ester with a tetraester of a methylenebisphosphonate to form a 3-alkenylidene-l,l-bisphosphonate containing an alkene moiety located gamma , delta to the phosphonates.