One-pot diversification approach can provide a new route to well-established drugs that have a large market size. For example, Indacaterol 2 is a long-acting beta-adrenoceptor agonist developed by Novartis. Its enantioselective synthesis involves laborious construction of the chiral aminoalcohol motif from 8-hydroxyquinoline 39, resulting in a 9-step synthesis (longest linear sequence). Instead, by just "attaching" the key aminoalcohol motif 11 to readily accessible heteroaryl iodide 36, the synthesis was considerably truncated to 5 steps. The routes to Salmeterol 3 and Vilanterol 47, widely used bronchodilators, can be similarly simplified. Due to their structural similarity, a divergent synthesis of these two top-selling drugs was envisioned using