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An effective method for bisphosphonate moiety inserting into O–H bond of carboxylic acids by Cu (II) catalyst

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Abstract In this study we developed a novel copper-catalyzed O–H insertion of tetraethyl diphosphonodiazomethane into carboxylic acids, providing a simple method to link bisphosphonates to compounds containing carboxyl group. Moreover,… Click to show full abstract

Abstract In this study we developed a novel copper-catalyzed O–H insertion of tetraethyl diphosphonodiazomethane into carboxylic acids, providing a simple method to link bisphosphonates to compounds containing carboxyl group. Moreover, a novel bone-targeting prodrug of naproxen was synthesized according to this new methodology, and the preliminary evaluation indicated that the prodrug exhibited excellent bone affinity in vitro .

Keywords: moiety inserting; inserting bond; carboxylic acids; effective method; method bisphosphonate; bisphosphonate moiety

Journal Title: Tetrahedron Letters
Year Published: 2018

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