1078733-84-2Relevant academic research and scientific papers
Palladium-catalyzed dehydrogenative coupling of cyclic enones with thiophenes: A rapid access to β-heteroarylated cyclic enones
Wen, Zhen-Kang,Song, Ting-Ting,Liu, Yu-Fang,Chao, Jian-Bin
, p. 3668 - 3671 (2018/04/12)
Dehydrogenative coupling of cyclic enones with heteroarenes has been a longstanding challenge because of the competitive ketone dehydrogenation and conjugated addition. Herein, a dehydrogenative coupling reaction of cyclic enones of different sizes with substituted thiophenes to construct β-thienyl cyclic enone compounds through palladium-catalyzed C-H functionalization under mild reaction conditions is reported. Simple substituted thiophenes with different functional groups can be directly introduced into cyclic enones with predominant regioselectivity at the α position of thiophene moieties and excellent functional group tolerance. Further molecular transformations of the coupling products to synthetically useful meta-heteroarylated phenol derivatives have also been demonstrated.
17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
-
Page/Page column 35, (2011/04/14)
The invention relates to 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) inhibitors, the preparation thereof and the use thereof for the treatment and prophylaxis of hormone-related, especially estrogen-related or androgen-related, diseases.
New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: Influence of additional substituents on 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitory activity and selectivity
Bey, Emmanuel,Marchais-Oberwinkler, Sandrine,Negri, Matthias,Kruchten, Patricia,Oster, Alexander,Klein, Tobias,Spadaro, Alessandro,Werth, Ruth,Frotscher, Martin,Birk, Barbara,Hartmann, Rolf W.
experimental part, p. 6724 - 6743 (2010/04/05)
17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is responsible for the catalytic reduction of weakly active E1 to highly potent E2. E2 stimulates the proliferation of hormone-dependent diseases via activation of the estrogen receptor α (ERα). Because o
Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1)
Bey, Emmanuel,Marchais-Oberwinkler, Sandrine,Werth, Ruth,Negri, Matthias,Al-Soud, Yaseen A.,Kruchten, Patricia,Oster, Alexander,Frotscher, Martin,Birk, Barbara,Hartmann, Rolf W.
experimental part, p. 6725 - 6739 (2009/11/30)
17β-Estradiol (E2), the most potent female sex hormone, stimulates the growth of mammary tumors and endometriosis via activation of the estrogen receptor α (ERα). 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1), which is responsible for the catalytic r
