Fluorinated block

In small-molecule drug discovery, the value of a molecular building block depends not only on whether its structure is novel, but also on whether it can be effectively introduced into target molecules and provide well-defined variables for structural optimization.

The pentafluorosulfanyl (SF₅) group, as a unique fluorine-containing functional group, has demonstrated broad application prospects in medicinal chemistry, materials science, and other fields due to its excellent chemical stability, high electronegativity, and lipophilicity. In recent years, ...

Pentafluorosulfanyl chloride (SF₅Cl), a pivotal reagent for direct pentafluorosulfanylation, has seen remarkable advancements in synthesis and handling safety. Key developments include

In 2015, the Dolbier group reported a method where phenylacetylene is used as the substrate, reacting with SF₅Cl under the catalysis of triethylborane (BEt₃) to generate a chlorinated pentafluorosulfanylated intermediate (189).

The introduction of highly fluorinated groups in drug and pesticide candidate compounds is a powerful strategy to modulate their properties. The introduction of fluorinated side chains can modulate acid-base and lipophilicity, impart a dipole moment, lock confirmation, and mitigate undesirable ...