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General approach to the synthesis of prochiral precursors of chiral atropisomeric biaryls based on several complementary methods has been developed. Biaryls were obtained in good to excellent yields depending on their structure and selected method of synthesis. Furthermore, we demonstrate a possibility of utilisation of the obtained compounds possessing 2 or 3  ortho  substituents around the aryl-aryl bond in direct and directed arylation reaction leading through transition metal-mediated C–H bond activation to atropisomeric compounds.

General Approach to the Synthesis of Prochiral Atropisomeric Biaryls