A highly efficient method for the preparation of a chiral 3,5-substituted pyrrolidinone will be described. The synthesis highlights a convergent multi-component coupling to the core of the molecule, followed by hydrolysis, dynamic kinetic resolution, and reductive amination. The steps of the synthesis and the overall process design strategy are highlighted, which include route selection criteria for a long-term manufacturing process. The strategy to control a problematic genotoxic impurity is also discussed.

Process development and synthetic approaches for a CB1 inverse agonist

248th National Meeting (2014)

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