Issue 32, 2019

Functional bisphosphonate synthesis for the development of new anti-resorption bone drug candidates

Abstract

Herein we present the synthesis of β-mono and β-bis-substituted vinylidenebisphosphonate esters bearing a carboxylic ester moiety to be used as building blocks for further functionalizations. Reactions of these new bisphosphonate scaffolds through hydrogenation of the unsaturated C[double bond, length as m-dash]C bond and through metal mediated addition of aryl boronic acids and indoles provide a wide range of new bisphosphonate products as potential leads to contrast osteoporosis.

Graphical abstract: Functional bisphosphonate synthesis for the development of new anti-resorption bone drug candidates

Supplementary files

Article information

Article type
Paper
Submitted
14 May 2019
Accepted
16 Jul 2019
First published
18 Jul 2019

New J. Chem., 2019,43, 12641-12649

Functional bisphosphonate synthesis for the development of new anti-resorption bone drug candidates

E. Bortolamiol, A. Chiminazzo, L. Sperni, G. Borsato, F. Fabris and A. Scarso, New J. Chem., 2019, 43, 12641 DOI: 10.1039/C9NJ02504A

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