[摘要]:The stereocontrolled total synthesis of largazole was accomplished starting from 3-[(tert-butyldimethylsilyl)oxy]propanol in 5.8% overall yield, unambiguously confirming its structure. Key steps included the use of the Nagao thiazolidinethione auxiliary for a diastereoselective acetate aldol reaction, thiazoline-thiazole formation, and macrolactamization by use of the Mukaiyama reagent.