Enantioselective Fluorination of α-Substituted β-Diketones Using β,β-Diaryl Serines

Org Lett. 2022 Jan 14;24(1):420-424. doi: 10.1021/acs.orglett.1c04104. Epub 2021 Dec 21.

Abstract

We report the enantioselective fluorination of α-substituted β-diketones using β,β-diaryl serines as a primary amine organocatalyst. The reaction affords the corresponding fluorinated products in yields of 74 to 99% with excellent enantioselectivity (75-95% ee). Moreover, for synthetic applications, the diol, aldols, and the allylic fluoride were synthesized from 2a, maintaining excellent enantioselectivity (94% ee). The control experiment reveals that the CO2H group of the β,β-diaryl serines plays an important role in inducing the high enantioselectivity.

Publication types

  • Research Support, Non-U.S. Gov't