- Hydrosilanes are not always a reducing reagent: A ruthenium-catalyzed introduction of primary alkyl groups to electron-rich aromatic rings using esters as a source of the alkyl groups
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A triruthenium cluster, (μ3, η2, η3, η5-acenaphthylene)Ru3(CO) 7 effectively catalyzes primary-alkylation reaction of electron-rich aromatic rings using a combination of hydrosilane and est
- Nagashima, Hideo,Kubo, Yuichi,Kawamura, Mitsunobu,Nishikata, Takashi,Motoyama, Yukihiro
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supporting information; experimental part
p. 7667 - 7672
(2011/10/19)
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- B(C6F5)3: an efficient catalyst for reductive alkylation of alkoxy benzenes and for synthesis of triarylmethanes using aldehydes
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Tris(pentafluorophenyl)borane [B(C6F5)3] has been used as an efficient catalyst for reductive alkylation of alkoxy benzenes using aldehydes as an alkylating agent in the presence of polymethylhydrosiloxane (PMHS). Various alkylated trimethoxybenzene derivatives have been prepared in good to high yields. In addition, B(C6F5)3 was also used as a catalyst for the reaction of electron-rich arenes with aldehydes to obtain triarylmethanes. The use of reductive alkylation protocol for the synthesis of an isochroman and tetrahydroisoquinoline derivatives has also been demonstrated.
- Chandrasekhar,Khatun, Sanjida,Rajesh,Raji Reddy
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experimental part
p. 6693 - 6697
(2010/01/18)
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- Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen receptors α and β
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In search of therapeutic agents for estrogen-related pathologies, phytoestrogens are being extensively explored. In contrast to naringenin, 8-prenylnaringenin is a potent hop-derived estrogenic compound, highlighting the importance of the prenyl group for hormonal activity. We investigated the effects of substituting the prenyl group at C(8) with alkyl chains of varying lengths and branching patterns on estrogen receptor (ER) subtype ERα- and ERβ-binding affinities and transcriptional activities. In addition, features of the ligand-induced receptor conformations were explored using a set of specific ER-binding peptides. The new 8-alkylnaringenins were found to span an activity spectrum ranging from full agonism to partial agonism to antagonism. Most strikingly, 8-(2,2-dimethylpropyl)naringenin exhibited full agonist character on ERα, but pronounced antagonist character on ERβ. Knowledge on how ER-subtype-selective activities can be designed provides valuable information for future drug or tool compound discovery.
- Roelens, Frederik,Heldring, Nina,Dhooge, Willem,Bengtsson, Martin,Comhaire, Frank,Gustafsson, Jan-?ke,Treuter, Eckardt,De Keukeleire, Denis
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p. 7357 - 7365
(2007/10/03)
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