Cu(I)-Catalyzed Enantioselective Alkynylation of Thiochromones

Org Lett. 2020 Feb 7;22(3):1155-1159. doi: 10.1021/acs.orglett.0c00005. Epub 2020 Jan 21.

Abstract

A highly efficient asymmetric synthesis of chiral thiochromanones is developed via Cu(I)/phosphoramidite catalyzed asymmetric alkynylation of thiochromones under mild reaction conditions. The catalyst system is tolerant of various thiochromone precursors and terminal alkynes. The established asymmetric transformation provides different enatiomeric-enriched thiochromanones with more molecular complexity and enables access to chiral thioflavanones, a subgroup of flavonoid by further functionalization.

Publication types

  • Research Support, Non-U.S. Gov't