Recent applications of C–H functionalization in complex molecule synthesis

Chen, K., Lei, X.
Current Opinion in Green and Sustainable Chemistry 2018, 11, 9–14

We have witnessed the striking advancement of C–H functionalization in organic synthesis over the past decade. This short review spotlights the very recent applications of C–H functionalization in natural product synthesis and drug synthesis. Some representative examples of natural product total synthesis facilitated by C–H functionalization are classified by C–O, C–C, C–N or C–X bond formation. Three different total syntheses are highlighted in details, in which iterative C–H functionalization strategy is involved. Another example of Merck's synthesis of anacetrapib is also discussed to briefly demonstrate the broad application of C–H functionalization strategy in process chemistry of pharmaceutical industry.

We have witnessed the striking advancement of C–H functionalization in organic synthesis over the past decade. This short review spotlights the very recent applications of C–H functionalization in natural product synthesis and drug synthesis. Some representative examples of natural product total synthesis facilitated by C–H functionalization are classified by C–O, C–C, C–N or C–X bond formation. Three different total syntheses are highlighted in details, in which iterative C–H functionalization strategy is involved. Another example of Merck's synthesis of anacetrapib is also discussed to briefly demonstrate the broad application of C–H functionalization strategy in process chemistry of pharmaceutical industry.