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Updated: Jun 1, 2025

Synthesis of a Borylated Ibuprofen Derivative Through Suzuki Cross-Coupling and Alkene Boracarboxylation Reactions
Published on: November 30, 2022
Iridium-catalysed C-H borylation of β-aryl-aminopropionic acids
Henry Robinson1, Joe Stillibrand1, Klemensas Simelis1
1GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry, University of Nottingham, Triumph Road, Nottingham, NG7 2TU, UK. andrew.nortcliffe@nottingham.ac.uk.
Abstract:
Iridium-catalysed catalytic, regioselective C-H borylation of β-aryl-aminopropionic acid derivatives gives access to 3,5-functionalised protected β-aryl-aminopropionic acid boronates. The synthetic versatility of these new boronates is demonstrated through sequential one-pot functionalisation reactions to give diverse building blocks for medicinal chemistry. The C-H borylation is also effective for dipeptide substrates. We have exemplified this methodology in the synthesis of a pan αv integrin antagonist.
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