Enantioselective synthesis achieves tetracyclic structure of citrifelin A, suggesting a new method for complex molecules.
The enantioselective first total synthesis of (-)-citrifelin A is described herein. We found that the oxa-Pictet-Spengler reaction and acid-promoted dihydropyran formation were effective for the stereocontrolled construction of the tetracyclic framework of 1. Starting from known materials, (-)-citrifelin A was synthesized in an eight-step longest linear sequence (LLS) with an overall yield of 17%.
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Hori et al. (2026) studied this question.
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