Ligand (biochemistry)

Pathology

Receptor

Organic chemistry

Combinatorial chemistry

Reactivity (psychology)

Stereochemistry

Enantioselective synthesis

Catalysis

Atropisomer

Stereoselectivity

Chemistry

Quinoline

Alternative medicine

Phosphoric acid

Biochemistry

Medicine

Angewandte Chemie International Edition

The discovery of proper ligands to simultaneously modulate the reactivity and effectively control the stereoselectivity is a central topic in the field of enantioselective C−H activation. Herein, we reported the synthesis of axially chiral biaryls by Pd‐catalyzed atroposelective C−H olefination. A novel chiral spiro phosphoric acid, STRIP, was identified as a superior ligand for this transformation. A broad range of axially chiral quinoline derivatives were synthesized in good yields with excellent enantioselectivities (up to 98 % ee ). Density functional theory was used to gain a theoretical understanding of the enantioselectivities in this reaction.

Enantioselective Synthesis of Biaryl Atropisomers by Pd‐Catalyzed C−H Olefination using Chiral Spiro Phosphoric Acid Ligands