De novo Synthesis of Fluoroarenes and Fluoro(hetero)arenes

Historically, one of the biggest challenges in synthetic organic chemistry has always been to synthesize fluoroarenes (Ar-F) and fluoroheteroarenes (Het-F) from cheap, readily available starting materials, as fluorination has always concerned synthetic chemists due to either undesirable safety of reagents, low selectivities or poor reactivities.

Since fluoroaryl- (Ar-F) and fluoroheteroaryl- (Het-F) are the most common fluorinated motives among pharmaceuticals development of a completely novel synthetic strategy would be of great importance to the research community. De novo construction of fluorobenzene using C1F1 synthons is an unprecedented process.

We foresee that little explored monofluorinated ortoformates (RO)3CF (FOFs) could be a synthetic equivalent to access C1F1 synthon for annulation reactions.