LATE-STAGE FUNCTIONALIZATION OF C—H BONDS IN ORGANIC SYNTHESIS

The development of new strategies for the functionalization of the historically inert C—H bond arises as an excellent way to create new carbon—carbon and carbon— heteroatom bonds. With increasingly chemo- and site-selective methods that enables the late-stage functionalization of C—H bonds, the modification of specific sites in natural products and pharmaceuticals without altering their scaffold emerges as a powerful means for the diversification of complex molecules. In this review, we will introduce concepts of late-stage modifications, the use of C—H bond functionalization to forge new carbon—carbon and carbon—heteroatom bonds using metal catalysis and photochemistry in simple examples and their applications in natural products and pharmaceuticals. The aim of the review is to update and display to the reader the contributions and implications of this methodology to organic synthesis.

Keywords:
C—H bond functionalization; late-stage functionalization; metal catalysis; natural products; pharmaceuticals