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Skeletal Modification via Activation of Relatively Unstrained C-C Bonds.

ConspectusMethods that can directly modify the skeletons of complex molecules have become increasingly attractive for preparing novel analogues without the need for de novo synthesis in drug discovery processes. Among the various skeletal modification approaches, those targeting unstrained C-C bonds are particularly challenging to realize, owing to the relative inertness of these bonds toward common reagents. Compared to C-H or C-X (X: heteroatom) bonds, the activation of unstrained C-C bonds is often not thermodynamically and/or kinetically favorable. As a result, strategies relying on highly