Angew Chem Int Ed Engl 2022 May 26. Epub 2022 May 26.
Wuhan University, College of Chemistry and Molecular Sciences, 299 Bayi Road, Wuchang, Wuhan, Hubei, China, 430072, 430072, Wuhan, CHINA.
1,3- trans -Disubstituted tetrahydroisoquinoline (THIQ) is a common heterocyclic structural unit of naphthylisoquinoline alkaloids. The assembly of this structural unit is not trivial, which constitutes a substantial challenge in the total synthesis of naphthylisoquinoline alkaloids and related pharmaceuticals. Herein, we report a modular and convergent method for the rapid assembly of 1,3- trans -disubstituted THIQ frameworks through a three-component Catellani reaction and a Au(I)-catalyzed cyclization/reduction cascade. Read More