From Industrial Method to the Use of Silylated P(III) Reagents for the Synthesis of Relevant Phosphonylated Molecules

Abstract

Phosphonates and their derivatives widely represent important pharmacophores in various classes of therapeutic agents from antivirals to antibiotics. Among these phosphonylated compounds, 1-hydroxymethylene-1,1-bisphosphonates (HMBPs) have occupied a very important place for 30 years now and are currently used in medicine for their inhibitory properties on bone resorption. HMBPs also exhibit direct and indirect antitumor effects in vitro against a broad variety of tumor cell lines, including melanoma, mesothelioma, prostate, breast, lung, and myeloma cancer cells. This review will discuss the various syntheses of bisphosphonates with the goal of illustrating their potential interest for the development of therapeutic agents. We will also disclose our latest achievements in phosphinate chemistry.