Rhodium‐Catalyzed Direct C7 Alkynylation of Indolines

An efficient rhodium(III)‐catalyzed direct C7 alkynylation of indoline CH bonds with the alkynylated hypervalent iodine reagents has been developed. This reaction proceeds smoothly under mild conditions over a wide structural scope with high site‐selectivity and excellent functional‐group tolerance. N ‐Acetyl as well as other N ‐acyls served as effective directing groups (DG). This procedure allows for the synthesis of a variety of 7‐alkynyl‐substituted indolines in good to excellent yield. More significantly, C7‐alkynylated indoles through further transformations have been successfully accessed. magnified image