Abstract
AbstractA concise synthesis of racemic Tapentadol and its stereoisomers was presented. The key step was a TiCl4·THF2‐catalzyed aza‐Belluš‐Claisen rearrangement to create two vicinal tertiary carbon stereogenic centers. The subsequent reduction of amide and hydrogenation of alkene delivered Tapentadol and its stereoisomers. The current approach offers a practical synthetic route to access this class of pharmaceutically significant molecules.
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