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Total Synthesis of Echinomycin and Its Analogues

Keita Kojima, Fumika Yakushiji, Akira Katsuyama, Satoshi Ichikawa

2020Organic Letters18 citationsDOI

Abstract

The first total synthesis of echinomycin (1) was accomplished by featuring the late-stage construction of the thioacetal moiety via Pummerer rearrangement and simultaneous cyclization, as well as two-directional elongation of the peptide chains to construct a C2-symmetrical bicyclic octadecadepsipeptide bridged with a sulfide linkage. This strategy can be applicable to a variety of echinomycin analogues.

Topics & Concepts

ChemistryMoietyStereochemistryBicyclic moleculeTotal synthesisPummerer rearrangementThioacetalCombinatorial chemistryOrganic chemistryAcetalCatalysisAcetic anhydrideMicrobial Natural Products and BiosynthesisChemical Synthesis and AnalysisSynthetic Organic Chemistry Methods
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