Combining asymmetric catalysis with natural product functionalization through enantioselective alpha-fluorination

将不对称催化与天然产物功能化通过对映选择性α-氟化相结合

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Abstract

An examination into the derivatization of various natural products using newly developed alpha-fluorination methodology is disclosed. An activated ketene enolate, generated from an acid chloride, is allowed to react with an electrophilic fluorine source (NFSi). Quenching the reaction with a nucleophilic natural product produces biologically relevant alpha-fluorinated carbonyl derivatives of select chemotherapeutics, antibiotics, and other pharmaceuticals.

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