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It has been extracted and processed since the dawn of civilization. All these features render iron a noncontaminant, biocompatible, nontoxic, and inexpensive metal and therefore it constitutes the perfect candidate to replace noble metals (rhodium, palladium, platinum, iridium, etc.). Moreover, direct C\u2212H functionalization is one of the most efficient strategies by which to introduce new functional groups into small organic molecules. The majority of organic compounds contain C(sp<jats:sup>3<\/jats:sup>)\u2212H bonds. Given the enormous importance of organic molecules in so many aspects of existence, the utilization and bioactivity of C(sp<jats:sup>3<\/jats:sup>)\u2212H bonds are of the utmost importance. This review sheds light on the substrate scope, selectivity, benefits, and limitations of iron catalysts for direct C(sp<jats:sup>3<\/jats:sup>)\u2212H bond activations. 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