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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 49, 2019 - Issue 24
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Synthetic Communications Reviews

A novel hydroxy-bisphosphonic acid prodrug as a candidate for the delivery of ibuprofen to bone

Sameh AounOrganic Chemistry Department, Université Libre de Tunis, Tunis, TunisiaCorrespondence[email protected]
&
Haythem BennourOrganic Chemistry Department, Université Libre de Tunis, Tunis, Tunisia
Pages 3412-3418 | Received 31 Jul 2019, Published online: 07 Oct 2019
 
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Abstract

Active targeting with controlled delivery of anti-inflammatory drugs to the bone is not sufficiently explored. In this study, concise and novel synthesis of a hydroxy-bisphosphonic acid (HBPA) prodrug containing ibuprofen is described. The key step consisted of preparing the HBPA function from a carboxylic acid precursor, in mild conditions and using appropriate Arbuzov reactions with tris(trimethylsilyl)phosphite. This prodrug would be an excellent candidate for the treatment of bone inflammation diseases such as rheumatoid arthritis.

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