A Comprehensive Review for the Straightforward Preparation of Trifluoromethylated Internal Alkynes

ABSTRACT Trifluoromethylated internal alkynes are presented as a class of versatile building blocks for efficient assembly of various trifluoromethyl group‐containing useful organic molecules through either direct nucleophilic addition or cyclization. Therefore, it has attracted significant attention from organic synthetic chemists and tremendous efforts have been devoted to the development of its rapid preparation. In this review, we aim to provide a comprehensive summary of the latest advances in the straightforward preparation of trifluoromethylated internal alkynes. We would also like to spur the recent discoveries and developments of innovative reaction paradigms in this field. Additionally, crucial challenges and future perspectives on this hot topic are also discussed, with the wish to provide a profound insight for not only future organofluorine chemistry but also fluorine‐containing pharmaceutical science. This manuscript mainly focuses on the direct synthetic methodology to construct various unsymmetrical trifluoromethylated internal alkynes, and it is categorized according to various synthetic methods as well as different types of trifluoromethyl source.