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European Journal of Organic Chemistry· 2026Q2· Review

Recent Synthetic Approaches and Future Prospects of Trifluoroacetyl Compounds

Pengting Han, Yu Zhong, Xinyu Wang, Dianhu Zhu

Short summary

Direct trifluoroacetylation using readily available reagents offers a more straightforward synthetic route to trifluoroacetyl-containing compounds compared to indirect methods.

AI-generated from the title and abstract; the full text is not read.

Key points

  • Direct trifluoroacetylation is a more straightforward approach than indirect methods.
  • Review covers indirect methods (e.g., oxidation of trifluoromethyl carbinols).
  • Review details direct methods using electrophilic, radical, and building-block reagents.
  • The aim is to guide synthetic chemists and identify future research opportunities.

AI-generated from the title and abstract; the full text is not read.

Abstract

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.

The authors' abstract, as published at the source. European Journal of Organic Chemistry, 2026 · DOI ↗

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Field: Pharmaceutical Science

Pharmaceutical SciencePharmacology, Toxicology and Pharmaceutics