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.
View Article and Find Full Text PDFContext: Bans on gender-affirming care (GAC) for transgender and gender-expansive (TGE) people are grounded in scientific disinformation and have been challenged in American courts.
Methods: Five legal filings by state officials in defense of GAC restriction from initial litigation were analyzed using reflexive thematic analysis. Themes and subthemes of disinformation were identified after review and analysis of these filings.
A late-stage functionalization of the aromatic ring in amino acid derivatives is described. The key step is a copper-catalysed diversification of a boronate ester by amination (Chan-Lam reaction) that can be carried out on a complex β-aryl-β-amino acid scaffold. This not only considerably extends the substrate scope of amination partners, but also delivers an array of potent and selective integrin inhibitors as potential treatment agents of idiopathic pulmonary fibrosis (IPF).
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