138743-03-0Relevant articles and documents
Process for the preparation of estetrol
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, (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.
15Alpha-substituted estradiol carboxylic acid esters as locally active estrogens
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Page/Page column 2; 6; sheet 2, (2010/02/08)
The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 15α-estradiol ester compounds is presented which exhibit excellent biologica
SYNTHESIS OF ESTETROL VIA ESTRONE DERIVED STEROIDS
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Page 25-26, (2008/06/13)
A process is provided for the making of estetrol starting from a 3-A-oxy-estra 1,3,5(10),15-tetraen-17-one, wherein A is an C1-C5 alkyl group, preferably a methyl group, or a C7 - C12 benzylic group, preferably a benzyl group. This process is particularly suitable to industry.
Synthesis and evaluation of B-, C-, and D-ring-substituted estradiol carboxylic acid esters as locally active estrogens
Labaree, David C.,Zhang, Jing-Xin,Harris, Heather A.,O'Connor, Craig,Reynolds, Toni Y.,Hochberg, Richard B.
, p. 1886 - 1904 (2007/10/03)
We have synthesized derivatives of estradiol that are structurally modified to serve as "soft" estrogens and act within a geographically limited area of the body; estrogens without systemic action. We have previously shown with 16α-substituted analogues o
SYNTHESIS OF 17β-ESTRADIOL DERIVATIVES WITH N-BUTYL, N-METHYL ALKYLAMIDE SIDE CHAIN AT POSITION 15
Poirier, Donald,Merand, Yves,Labrie, Fernand
, p. 7751 - 7766 (2007/10/02)
New derivatives of 17-β-estradiol with N-butyl, N-methyl alkylamide side chains of three different lengths at position 15 have been synthesized from estrone.Compounds 5 and 6 having a shorter alkylamide chain were obtained in eleven steps by introduction