Copper‐Catalyzed Chemoselective Divergent Carbene Insertion into the N−H bonds of Tryptamines.

Easy access to divergent products with chemoselectivity is of great importance in organic synthesis. Herein, we have developed a chemoselective copper‐catalyzed carbene insertion protocol onto N−H bonds of tryptamine derivatives. Divergent insertion products are obtained by varying the nucleophilicity of the aliphatic NH of tryptamine with electron‐donating or electron‐withdrawing groups. The reaction provided N−H insertion products with broad substrate scope in good yields. [ABSTRACT FROM AUTHOR]