Isoxazole group directed Rh(III)-catalyzed alkynylation using TIPS-EBX.

A highly effective isoxazole directed ortho C-H alkynylation has been developed. Rhodium(III) catalyzed direct di-(and/or mono) alkynylation using a hypervalent iodine reagent (TIPS-EBX) is reported. The reaction proceeds with a wide substrate scope under benign conditions. Preliminary mechanistic studies support this chelation assisted C-H alkynylation.