Ethynyl estradiol (I) was protected at the phenolic hydroxyl group as the silyl ether (II) by using triethylsilyl chloride and imidazole. The lithium acetylide derived from (II) was then carboxylated by a stream of CO2 to afford the propiolic acid derivative (III). Subsequent coupling of acid (III) with the cyclic enediine alcohol (IV) in the presence of EDC and DMAP furnished the silyl-protected ester (V). Finally, desilylation of (V) with either Bu4NF or HF穚yridine led to the target compound.