Macrocyclic natural products play an important role in drug discovery. Recently, synthetic macrocycles have attracted considerable interest from organic and medicinal chemists because of their unique physiochemical properties. Macrocyclic chemotypes have been utilized as an alternative to conventional small molecules, especially for “non-druggable” targets including protein-protein interaction surfaces. We have discovered an efficient approach to C-C bond-forming macrocycle construction. Modular sulfonylhydrazone substrates have been constructed which can be cyclized to 13-20 member rings in an efficient manner. A broad substrate scope and good functional group tolerance have been demonstrated. In addition, post-functionalization of macrocycles for further diversification has been investigated.

C-C bond-forming macrocyclization using modular sulfonylhydrazone substrates

256th National Meeting (2018)

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