Facile solid-phase construction of indole derivatives based on a traceless, activating sulfonyl linker

[GRAPHICS] Palladium-mediated coupling/intramolecular indole cyclization of terminal a lkynes with resin 8, followed by cleavage of the sulfonamide linkage, were executed under mild conditions to provide diverse indoles 10 in excellent y ield and purity. This chemistry benefits from a dual activation process tha t derives from use of a traceless N-sulfonyl linker. Also, direct mercurati on of 9 (X = H, R = 4-Me-C6H4), followed by palladium mediated coupling wit h methyl acrylate, efficiently provided I functionalized product 12.