Article ID Journal Published Year Pages File Type
5220418 Tetrahedron 2011 5 Pages PDF
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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Physical Sciences and Engineering Chemistry Organic Chemistry
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