Our approach for the synthesis of the EGCG 10 substituted at the C8 position of the A ring is based on an electrophilic substitution of the protected EGCG 12 with the amidomethyl 2-alkynylbenzoate 11. Treatment of the amidomethyl 2-alkynylbenzoate 11 with (Ph3P)AuOTf under neutral conditions generates the N-acyl imine 13 along with the coumarin 6. The N-acyl imine 13 can react with the protected EGCG 12 at the electron-rich 8 position of the A ring. The method could directly incorporate acidically and basically sensitive functional groups to EGCG.