213819-19-3Relevant academic research and scientific papers
Process for the preparation of estetrol
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Page/Page column 19, (2011/11/12)
The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3,15α,16α,17β-tetraol (estetrol), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, wherein A is a protecting group and B is ―Si(R2)3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10),15-tetraen-17-one, wherein A is a protecting group, via said silyl enol ether derivative.
Methyl hypofluorite in the synthesis of 16-methoxyestradiol stereoisomers
Jonson, Stephanie D.,D'Avignon, D. Andre,Katzenellenbogen, John A.,Welch, Michael J.
, p. 470 - 478 (2007/10/03)
The unusual chemistry of methyl hypofluorite provides a previously unexplored route for functionalizing the 16-position of estradiol. Three isomers of 16-methoxyestradiol were prepared via two synthetic routes, each using methyl hypofluorite. The estrogen
