Recent Synthetic Approaches and Future Prospects of Trifluoroacetyl Compounds

The incorporation of a trifluoroacetyl group into drug candidates has emerged as an indispensable strategy in modern pharmaceutical research. In contrast to cumbersome indirect methods, direct trifluoroacetylation using readily available reagents provides a more straightforward route. This review provides a comprehensive and critical overview of all synthetic avenues to trifluoroacetyl‐containing compounds, encompassing both indirect approaches (e.g., oxidation of trifluoromethyl carbinols) and direct methods using electrophilic, radical, and building‐block‐type trifluoroacetylating reagents. This review aims to serve as a comprehensive decision‐making guide for synthetic chemists and to highlight underexplored areas ripe for future methodological innovation.