Ligand-enabled cross-coupling of C(sp3)–H bonds with arylboron reagents via Pd(II)/Pd(0) catalysis

摘要: There have been numerous developments in C-H activation reactions the past decade. Attracted by ability to functionalize molecules directly at ostensibly unreactive bonds, chemists discovered reaction conditions that enable of C(sp(2))-H and C(sp(3))-H bonds with a variety coupling partners. Despite these advances, development suitable ligands catalytic bond functionalization remains significant challenge. Herein we report discovery mono-N-protected amino acid ligand enables Pd(II)-catalysed γ-C(sp(3))-H triflyl-protected amines arylboron reagents. Remarkably, no background was observed absence ligand. A amine substrates reagents were cross-coupled using this method. Arylation optically active derived from acids also provides potential route for preparing non-proteinogenic acids.