Tetrahedron Letters p. 7027 - 7030 (1999)
Update date:2022-08-04
Topics:
Couladouros, Elias A.
Moutsos, Vassilios I.
A general synthetic route for the construction of the western part of the macrocyclic bastadins 4-16 is presented. The western and the eastern segments were coupled using the imidazolide of the corresponding acid. The bromine at position Y2 may be added at this advanced step regiospecifically, strengthening the convergence of the presented approach. Finally, the fully functionalized α,ω-aminoacid is cyclized with EDC affording the macrocyclic ring of bastadin-12 in 72% yield (3.5% overall yield).
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