A highly efficient and step-economical synthesis of zincophorin methyl ester has been achieved. The unprecedented step economy of this zincophorin synthesis is principally due to an application of the tandem silylformylation鈥揷rotylsilylation/Tamao oxidation鈥揹iastereoselective tautomerization reaction, which achieves in a single step what would typically require a significant multistep sequence.