Short synthesis of 2-methoxyestradiol and 2-hydroxyestradiol |
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| Authors: | Kiuru Paula S Wähälä Kristiina |
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| Institution: | Department of Chemistry, Organic Chemistry Laboratory, University of Helsinki, A. I. Virtasen aukio 1, P.O. Box 55, FIN-00014 Helsinki, Finland. |
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| Abstract: | The estrogen metabolite 2-methoxyestradiol was synthesized from estradiol bis-THP-ether which was 2-hydroxylated using the superbase LIDAKOR, trimethyl borate, and H(2)O(2), then methylated and deprotected to obtain 2-methoxyestradiol in three steps and 61% yield. 2-Hydroxyestradiol was obtained by deprotecting the 2-hydroxyestradiol bis-THP-ether from the first step. |
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| Keywords: | Steroid Estrogens Synthesis Metabolites 2-Methoxyestradiol 2-Hydroxyestradiol |
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