Herein, a concise protocol for the construction of axially chiral biaryls via Pd-catalysed direct C-H arylation of 1-arylisoquinoline N-oxides through kinetic resolution using a commercially available, cost-effective, and bench-stable chiral mono-protected amino acid has been uncovered. The high conformational stability of the axially chiral products in different solvents and at high temperatures, as observed from the experimental studies and DFT calculations, shows their excellent stability.