Nickel-Catalyzed Cross-Coupling of Aziridines with Thioesters toward Atom-Economic Synthesis of β-Sulfanyl Amides

Abstract

Thioesters have been recognized as a class of powerful bifunctional reagents, namely, great donors of acyl and sulfide moieties. However, such application in value-added synthesis is still very limited to date. Herein, a nickel-catalyzed cross-coupling reaction system of aziridines with thioesters was developed under redox-neutral and mild conditions. This catalytic method provides an atom-economic route for the synthesis of diverse β-sulfanyl amide derivatives with wide substrate scope (43 examples), good functional group tolerance, and regioselectivity.β-Sulfanyl amides are one of the most valuable scaffolds that are widely distributed in a large number of naturally occurring products and bioactive molecules, such as Nelfinavir, Penicillin, Zofenopril, and Temocapril (Figure 1). 1 Consequently, the