Asymmetric Total Synthesis of (+)-Coprophilin

Abstract

In this paper, we report the first total synthesis of (+)-coprophilin, an anticoccidial agent, by constructing the chiral linear precursor via a Mukaiyama–Evans aldol reaction and a stereoselective intramolecular Diels–Alder reaction. The proposed method can be used to provide large amounts of (+)-coprophilin, which exhibits a 3,4,5,6,7-pentasubstituted Δ^1,2-octalin core structure.

Key words

total synthesis - stereoselective synthesis - antibiotics - Diels–Alder reaction - aldol reaction

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