14984-43-1Relevant articles and documents
NOVEL AND REGIOSPECIFIC SYNTHESIS OF 2-AMINO ESTROGENS VIA ZINCKE NITRATION
Numazawa, Mitsuteru,Kimura, Katsuhiko
, p. 675 - 682 (1983)
An efficient synthesis of 2-aminoestrone (14), 2-aminoestradiol (15), 2-amino-16α-hydroxyestrone (16) and 2-aminoestriol (17) is described. 2,4-Dibromo estrogens 1 - 4 were regiospecifically converted to the corresponding 2-nitro-4-bromo derivatives 5 - 8 in quantitative yields, with Zincke nitration using sodium nitrite.Catalytic hydrogenation of the 2-nitro-4-bromides 5 - 8 over palladium-on-charcoal gave directly the desired 2-amino estrogens 14 - 17 in high yields.The 2-amino compounds 15 and 17 were also obtained by the reduction of the corresponding 2-nitro-4-bromides 6 and 8 with sodium borohydride in the presence of palladium chloride.
COMPOUNDS, COMPOSITIONS, AND METHODS FOR TREATMENT OF ANDROGEN-MEDIATED DISEASE
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Paragraph 0137, (2020/05/28)
Provided herein are steroid sulfatase inhibitor compounds and androgen receptor inhibitor compounds that can be useful in, for example, the treatment of cancers such as prostate cancer and breast cancer. Pharmaceutical compositions and kits including the
Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors
Lawrence Woo,Leblond, Bertrand,Purohit, Atul,Potter, Barry V.L.
experimental part, p. 2506 - 2519 (2012/06/01)
Estrone sulfamate (EMATE) is a potent irreversible inhibitor of steroid sulfatase (STS). In order to further expand SAR, the compound was substituted at the 2- and/or 4-positions and its 17-carbonyl group was also removed. The following general order of p