Catalytic Generation of α-CF_3 Enolate: Direct Catalytic Asymmetric Mannich-Type Reaction of α-CF_3 Amide

摘要

The introduction of the CF_3 unit is a common strategy for modifying pharmacokinetic properties and slowing metabolic degradation in medicinal chemistry. A catalytic and enantioselective addition of α-CF_3 enolates allows for expeditious access to function-alized chiral building blocks with CF_3-containing stereo-genicity. To date, α-CF_3 enolates have been a less explored class of nucleophiles because of rapid defluorination. The present study reveals that a designed α-CF_3 amide enables a direct asymmetric Mannich-type reaction in a cooperative catalytic system.