Shenzhen Grubbs Institute and Department of Chemistry , Southern University of Science and Technology , Shenzhen 518055 , China.
Department of Chemistry , The Hong Kong University of Science & Technology , Clear Water Bay, Kowloon , Hong Kong.
Org Lett. 2020 Feb 7;22(3):1155-1159. doi: 10.1021/acs.orglett.0c00005. Epub 2020 Jan 21.
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.
发展了一种高效的手性硫色满酮不对称合成方法，通过温和的反应条件下，Cu(I)/手性膦酰胺催化硫色满酮的不对称炔基化反应实现。该催化剂体系对各种硫色满酮前体和末端炔烃具有耐受性。所建立的不对称转化提供了具有更多分子复杂性的不同对映体富集的硫色满酮，并通过进一步的官能化实现了类黄酮的一个亚组手性硫黄酮的获得。
