Domino Condensation/S‐Arylation/Heterocyclization Reactions: Copper‐Catalyzed Three‐Component Synthesis of 2‐N‐Substituted Benzothiazoles

All in it together: A highly efficient and extremely versatile method for the assembly of benzothiazoles with a nitrogen substituent in the 2-position relies on a copper-catalyzed cascade reaction of a 2-haloaniline, carbon disulfide, and an N nucleophile (see scheme). The products are useful precursors for the synthesis of a range of important pharmaceutical agents. DMF=N,N-dimethylformamide; R,R′=H, alkyl, aryl; Z=Me, CF3, CO2Me, CN, N2O, Cl, F, Ac.