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Hetereocycles are ubiquitous in nature and are widely present in drugs, natural products, biologically active compounds, and material science.They have been identified as privileged scaffolds in pharmaceuticals and agroehemieals.Therefore, tremendous efforts have been made to develop efficient methods to their synthesis.Herein, we reported our recent efforts in the expeditious synthesis of hetetreocycles via C-H activation based on two synthetic pathways: de novo synthesis and direct functionalization.