Efficient diastereoselective synthesis of (2R,3R,4R)-2-amino-3-hydroxy-4,5-dimethylhexanoic acid, the lactone linkage unit of homophymine A.

For the total synthesis of novel cyclodepsipeptide homophymine A, (2R,3R,4R)-2-amino-3-hydroxy-4,5-dimethylhexanoic acid was successfully synthesized by Evans' asymmetric alkylation and the anti-selective asymmetric hydrogenation of a chiral α-amino-β-keto ester as the key steps.