A Stereocontrolled synthesis of hapalosin

摘要

A facile synthetic method for two components of hapalosin,that is,betahydroxy-gamma-amino acid and beta-hydroxy acid,has been established by utilizing chiral building blocks efficiently resolved in a lipase-catalyzed transesterificantion.Furthermore,the synthesis of hapolosin through macrolactamization of the seco acid derived from these two components and (S)-2-hydroxy-3-mehtlbutyric acid has thus been demonstrated.