Concise enantioselective synthesis of (+)-sertraline and (−)-CP-52002 using proline catalysis

A short enantioselective synthesis of (+)-sertraline and its C4 epimer (−)-CP-52002 with an overall yield of 30%, respectively, as its hydrochloride has been described. The key steps are the proline catalyzed Mannich reaction of acetaldehyde and acid catalyzed intramolecular Friedel–Crafts’ alkylation reaction of olefin proceeding with high optical purities.