As the most electronegative element, fluorine has attracted enormous recent attention in the fields of agricultural and medicinal chemistry as well as In the materials science. Nowadays, the efficient and selective incorporation of fluorine atom(s) or fluorine-containing moieties into organic molecules to modulate their biological properties has become a routine and powerful strategy in drug design. Asymmetric fluorination and fluoroalkylation are two categories of most fascinating reactions in organofluorine chemistry, and the enantioselecttve electrophilic fluorination and enantioselective nudeophilic monofluoromethylation represent the state-of-the-art achievements." Currently, enantioselective trifluoromethylation and difluoromethylation are still very challenging topics regarding the stereoselectivity and generality, while the highly diastereo-selectlve trifluoromethylation and difluoromethylation have been achieved by using proper chiral auxiliaries.
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