Regioselective Copper-Catalyzed C-N and C-S Bond Formation Using Amines, Thiols and Halobenzoic Acids

Abstract

A regioselective method for highly efficient C-N and C-S bond formation with 2-halobenzoic acids is described. The Cu/Cu₂O-catalyzed reaction is carried out in 2-ethoxyethanol or ethylene glycol diethyl ether and does not require the use of strong base or other additives. This procedure eliminates the need for acid protection, tolerates a wide range of functional groups and provides aromatic­ and aliphatic amines and sulfides in 81-99% yield.

amines - thiols - halobenzoic acids - carbon-heteroatom bond formation

References

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