Gold-Catalyzed 1,2-Aminoarylation of Alkenes with External Amines

Reported herein is the gold-catalyzed 1,2-aminoarylation of alkenes that engages external amine as a coupling partner. Careful optimization studies revealed a significant role of the concentration of base to achieve highly chemoselective access to the aminoarylation products over potential C-N cross-coupled products. Overcoming all the limitations, the current strategy provided straightforward access to the medicinally relevant 3-aminochroman, 2-aminotetrahydronaphthalene, and 2-aminoindane derivatives.

Automated summary

The study reported a gold-catalyzed 1,2-aminoarylation of alkenes using external amines as coupling partners. By carefully optimizing the reaction conditions, the researchers were able to achieve highly chemoselective access to the desired aminoarylation products by controlling the concentration of base. This strategy provided straightforward access to medicinally relevant derivatives like 3-aminochroman, 2-aminotetrahydronaphthalene, and 2-aminoindane.