Enantioselective Total Synthesis of Citrifelin A via the Oxa-Pictet–Spengler Reaction and Acid-Promoted Dihydropyran Formation

Key Points

• The aim is to achieve the first total enantioselective synthesis of (-)-citrifelin A.
• Utilized the oxa-Pictet-Spengler reaction to construct the core structure.
• Employed acid-promoted dihydropyran formation for stereocontrol.
• Conducted an eight-step synthesis path for total synthesis.
• Started from known chemical materials.
• Achieved synthesis of (-)-citrifelin A with an overall yield of 17%.
• Successfully constructed the tetracyclic framework through specified reactions.

Abstract