Aliphatic systems are ubiquitous in numerous natural products and pharmacoactive compounds. Selective remote C–H functionalization of such aliphatic chains is of great significance and remains a challenge to be addressed. The native functional group assisted C(sp3)–H activation has come up as one of the most practical and simpler approaches to transforming aliphatic compounds as it eliminates the need for an external directing group, thereby making the process more step and atom economic. In this regard, aliphatic acids and amines have gained tremendous attention in the recent past due to the unique coordination abilities of carboxylate and amine groups with transition metals. We have summarized here all the concepts and applications reported in the remote C(sp3)–H functionalization of aliphatic systems in recent times. The systematic presentation here is expected to provide a deeper understanding to beginners as well as experts interested in this exciting search field.
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