Prior routes require multiple steps for the (hetero)arenes construction, cryogenic temperatures, and air-and moisturefree conditions. Figure illustrates three examples of this challenge, sourced directly from the medicinal chemistry patent literature. The first example involves the preparation of key intermediate 97, used to prepare several inhibitors of 5-lipoxygenase activating protein (FLAP). In the original route, the two arenes were installed on cyclobutanone 6 via Grignard addition, followed by Friedel-Crafts. A final Pd-catalyzed borylation afforded 97 in 9% overall yield. In contrast, sequential installation of 3-iodo-indole 92 and aryl iodide 94 via the current protocol led to the same product in 18% overall yield. This sequence not only offers higher yields but also enhances modularity, enabling the efficient coupling of electron-poor arenes that would typically be unreactive in traditional Friedel-Crafts alkylation. KIT (tyrosine kinase) inhibitor intermediate 102 was prepared in four steps with an overall yield of 0.1%. The low yield was primarily attributed to the poor conversion of the Pd-catalyzed arylation step and the inefficient oxetaneforming ring closure. The revised synthetic route simplifies the process starting from the a-bromoacid 14f and significantly increases the overall yield to 15%.