On January 27, 2011, Schwede, Wolfgang; Klar, Ulrich; Moeller, Carsten; Rotgeri, Andrea; Bone, Wilhelm published a patent.Category: ethers-buliding-blocks The title of the patent was 17-Hydroxy-17-pentafluoroethylestra-4,9(10)-dien-11-aryl derivatives as progesterone receptor antagonists and their preparation and use in the treatment of diseases. And the patent contained the following:
The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-dien-11-aryl derivatives of formula I exhibiting progesterone-antagonistic effects and to methods for the production thereof, to the use thereof for the treatment and/or prophylaxis of diseases and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases, in particular uterine fibroids (myomas, uterine leiomyomas), endometriosis, menorrhagia, meningiomas, hormone-dependent mammary carcinomas and menopause-associated troubles, or for fertility control and emergency contraception. Compounds of formula I wherein R1 is SH and derivatives, S(O)H and derivatives, SO2H and derivatives, SONH2 and derivatives, (un)substituted aryl, etc.; X is O, NOH and derivatives and NNHSO2H and derivatives; and stereoisomers, salts, solvates, solvated salts, and all crystal modifications thereof, are claimed. Example compound II was prepared by addition of pentafluoroiodoethane to (5’R,8’S,10’R,13’S,14’S)-5,5,13′-trimethyl-1′,2′,6′,7′,8′,12′,13′,14′,15′,16′-decahydro-17’H-spiro[1,3-dioxan-2,3′-[5,10]epoxycyclopenta[a]phenanthren]-17′-one, followed by conjugate addition of 1-bromo-4-methylthiobenzene in the presence of magnesium and copper, and deacetalization. All the invention compounds were evaluated for their progesterone receptor antagonistic activity. From the assay, it was determined that compound II exhibited IC50 values of 0.011 nmol/L and 0.012 nmol/L towards progesterone receptor A and B, resp. The experimental process involved the reaction of Benzyl(4-bromophenyl)sulfane(cas: 53136-21-3).Category: ethers-buliding-blocks
The Article related to estradiene aryl preparation progesterone receptor antagonist, Steroids: Estranes and other aspects.Category: ethers-buliding-blocks
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem