Abstract

AN EXHAUSTIVE METHODOLOGICAL REVIEW OF PATENTS ON THE SYNTHESIS AND PURIFICATION OF ZOLEDRONIC ACID

Sanjay Sukumar Saralaya*

Abstract

The present review work was focused on extracting the disclosed methods from patents about the synthesis and purification of Zoledronic acid. Numerous patents were filed by the researchers/organizations over the years to synthesize Zoledronic acid with significant claims. In most of the patents, synthesis and biological activities of a few related dronic acids are also demonstrated alongside Zoledronic acid. In the context, 1-H-imidazole, 1-H-imidazol-1-ylacetic acid, 1-H-imidazol-1-ylacetic acid hydrochloride were found to be the major key starting materials used to synthesize Zoledronic acid. Similarly, phosphoric acid/phoshorous acid and phoshorous trichloride/phosphorous oxychloride are the key P-reagents used for phosphorylation.

Keywords: Zoledronic acid, 1-H-imidazole, 1-H-imidazol-1-ylacetic acid, 1-H-imidazol-1-ylacetic acid hydrochloride, phosphorylation, hydrolysis, recrystallization.