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This review showcases a systematic overview of the available tools for the catalytic asymmetric transformation of biaryl substrates toward the construction of challenging enantioenriched helicenes and the conceptual aspects associated with each type of transformation. Depending on the properties of the biaryl and the nature of the process, several methodologies have been developed, including olefin metathesis, hydroarylation of alkynes, C–X (X = C, O, N) coupling, and C–H functionalization. Pioneering studies and an array of representative reactions are discussed to underscore the potential of these synthetic protocols.

Graphical abstract: Catalytic asymmetric construction of helicenes via transformation of biaryls

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