ortho-Formylation of estrogens. Synthesis of the anti-cancer agent 2-methoxyestradiol |
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| Authors: | Ø yvind W. AkselsenTrond Vidar Hansen |
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| Affiliation: | School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, PO Box 1068, Blindern, N-0316 Oslo, Norway |
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| Abstract: | Several estrogens were mono-formylated using a mixture of paraformaldehyde, MgCl2, and Et3N in refluxing THF. In all cases, the 2-isomer was formed as the major product with high regioselectivity compared to the 4-isomer. Excellent to high yields were obtained in all examples except one. The method was applied for an efficient synthesis of the anti-cancer agent 2-methoxyestradiol. |
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| Keywords: | ortho-Formylation Estrogens 2-Methoxyestradiol |
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