LAUSR

Ramelteon is the first medicine in human history that treat insomnia as a melatonin receptor agonist. Herein, we report an efficient three‐step synthetic route to access it from commercially available 2,3‐dihydrobenzofuran‐4‐amine, which represents as the shortest racemic synthesis to date with a 26 % overall yield. Key to the success is the application of the intermolecular Catellani‐type alkylation and intramolecular redox‐relay Heck cyclization cascade for preparation of the key indane‐containing aldehyde. The unique primary amide‐involved reductive amination of aldehyde is another feature of this route. New process of ramelteon can be developed based on this chemistry.