CF3-bearing aromatic and heterocyclic building blocks

A review. Fluorine remains an insiders' tip in the life sciences as it enables the fine-tuning of biol. properties. However, the synthesis of fluorine-substituted target compds. is not always trivial. Virtually any fluorine atom attached to an org. backbone has ultimately to be imported from inorg. sources. Crucial for the entire synthetic planning in medicinal and agricultural research is the decision on at what stage and how the halogen will be introduced. Std. tech. processes, in particular the displacement of chlorine using anhyd. hydrogen fluoride or potassium fluoride, can hardly be implemented rationally on the lab. scale. Universal methods that are applicable by both industrial and academic researchers thus have great appeal. If a trifluoromethyl-substituted arene or heterocycle is the target compd., two splendid options exist. The CF3 group can be delivered packagewise by coupling an appropriate substrate with in situ generated (trifluoromethyl)copper. Alternatively, one may start from a CF3-substituted arene or heterocycle as a core and complete it with the missing parts of the ultimate structure. [on SciFinder (R)]