Abstract: Considering C-H bond as functional group and using them as a potential diversification tool to generate new analogues of a lead structure, is a convenient way to improve drug discovery process. From providing better understanding of structure–activity relationship (SAR), selectivity and absorption–distribution–metabolism–excretion (ADME) properties to the improvement of physical properties such as solubility, stability, permeability etc., Late Stage Functionalization (LSF) provides better opportunity for medicinal chemist to explore the chemical scope efficiently than solely depending on conventional synthesis.

Although promising, the selectivity and purification problem imparts difficulties in the pharmaceutical application of these strategies. But the tremendous effort of synthetic chemist across the world, over the past decades have developed a deeper and clearer understanding of the important factors that are crucial for transition metal catalysed C-H functionalization, to provide innovative real-life solutions.


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