Asymmetric Total Synthesis of Hetiamacins A–F

[Image: see text] Herein, we report a concise and stereoselective approach for the asymmetric total synthesis of hetiamacins A–F on the basis of the total synthesis of amicoumacin C, which could be synthesized from a known l-aspartic acid derivative. The synthesis of hetiamacin A was accomplished by an 11-step sequence that featured 1,3-oxazinane ring formation of amicoumacin B followed by amidation in one pot. Hetiamacins B–F were synthesized from amicoumacin A in only one step.