Iridium-catalysed C–H borylation of β-aryl-aminopropionic acids

Iridium-catalysed catalytic, regioselective C-H borylation of beta-aryl-aminopropionic acid derivatives gives access to 3,5-functionalised protected beta-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 alpha(v)integrin antagonist.