Consecutive catalytic electrophilic fluorination/amination of β-keto esters: toward α-fluoro-α-amino acids?
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Add time:08/29/2019 Source:sciencedirect.com
Monofluorination of β-keto esters with Selectfluor® (1-chloromethyl-4-fluoro-1,4-diazoniabicyclo[2,2,2]octane bis(tetrafluoroborate)) using CpTiCl3 as a catalyst, followed by amination with diazodicarboxylates using a Cu/Ph-Box catalyst leads to α-fluoro-α-hydrazino-β-keto esters in good yields and good selectivities (ee up to 94%).
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