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Amamistatin A, a linear lipopeptide and a growth inhibitor of human tumor cell lines from an actinomycete, was efficiently synthesized by a convergent approach. The asymmetric synthesis of β-hydroxy acid fragment was achieved by using chiral oxazaborolidinone mediated aldol reaction. The oxazole ring was constructed from N-acylthreonine via side-chain oxidation and cyclodehydration. The synthesis...