No abstract

The α-alkylation of deprotonated Strecker products derived from primary amines and aromatic aldehydes with 2-halobenzyl halides furnishes intermediates that can be cyclized to 1,2-disubstituted indoles in moderate to high yields (up to 94% over two steps) by microwave-assisted copper- or palladium-catalyzed intramolecular cross-coupling.

The application of borylated N-aryl sulfoximines as newly designed synthetic building blocks in Suzuki-type cross coupling reactions offers rapid access to a wide range of N-biaryl derivatives with potential relevance for medicinal chemistry and crop protection in good to excellent yields (up to 98%).

Starting from NH‐sulfonimidamides, rhodium‐catalyzed C−H bond alkenylation followed by aza‐Michael cyclization leads to unprecedented benzoisothiazole 1‐oxides. The applicability and robustness of the method is demonstrated in 25 examples with yields up to 95 %. The resulting scaffolds are partly saturated, 3D heterocycles with potential significance for medicinal and agricultural chemistry.