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Regioselective synthesis of estrogens achieved.A convenient one-pot protocol was used that tolerates air and moist.Analogs of the steroid metabolite 2-methoxyestradiol were prepared as potential new anti-cancer agents.Some analogs showed anti-proliferative effects in the low micromolar range observed in the CEM and HeLa cell lines.The regioselective synthesis of estrogens and their derivatives continues to be of interest. Most reported syntheses require multistep protocols associated with poor overall yield and lack of regioselectivity. New preparative protocols are still desired. Herein, 11 2-alkylated 17β-estradiol analogs were synthesized in a highly regioselective manner. The products were obtained using a convenient, one pot and high-yielding protocol. The anti-proliferative activity of the compounds was tested in human T-cell leukemia (CEM), human cervix carcinoma (HeLa) and human dermal microvascular endothelial (HMEC-1) cells.