In the past decade, multiple catalytic C-H bond functionalization has been successfully applied in natural product synthesis as a strategy to reduce the number of steps, increase overall yield and employ more easily available starting materials. This minireview presents selected examples making use of multiple C-H bond functionalization in conceptually different ways. First, linear syntheses are discussed, wherein multiple C-H functionalization is employed either from simple (hetero)cyclic cores, at a late stage, or to build polycyclic systems. Second, the use of multiple C-H functionalization as a strategic tool in convergent synthesis to access and couple complex fragments is discussed. Information on the scalability of the employed methods is provided when available. The presented cases indicate that multiple C-H functionalization strategies should play a great role to shape the future synthesis of functional complex molecules with improved sustainability.
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