78007-35-9Relevant academic research and scientific papers
Copper(I)/DDQ-Mediated Double-Dehydrogenative Diels-Alder Reaction of Aryl Butenes with 1,4-Diketones and Indolones
Chen, Jie,Hu, Wei,Wang, Min,Xu, Wen-Lei,Zhao, Wei-Ming,Zhou, Ling
supporting information, p. 7169 - 7174 (2020/10/12)
A copper(I)/DDQ-mediated double-dehydrogenative Diels-Alder (DDDA) reaction of simple butenes with 1,4-diketones and indolones has been established for the first time. This strategy is based on a tandem double-dehydrogenation/Diels-Alder reaction from nonprefunctionalized starting materials, in which both a diene and dienophile were in situ generated via activation of fourfold inert C(sp3)-H bonds in one catalytic system.
Visible-light-induced Ci-S bond activation: Facile access to 1,4-diketones from β-ketosulfones
Xuan, Jun,Feng, Zhu-Jia,Chen, Jia-Rong,Lu, Liang-Qiu,Xiao, Wen-Jing
supporting information, p. 3045 - 3049 (2014/03/21)
A novel method for the synthesis of 1,4-diketones from β-ketosulfones was developed by means of a visible light-induced Ci£S bond activation process. Symmetrical and unsymmetrical 1,4-diketones can be easily prepared in moderate to good yields. A new and efficient method for the synthesis of 1,4-diketones from β-ketosulfones was developed by means of a visible-light-induced Ci£S bond activation process (see scheme). Symmetrical and unsymmetrical 1,4-diketones can be easily prepared in moderate to good yields.
Acylguanidine inhibitors of β-secretase: Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets
Cole, Derek C.,Stock, Joseph R.,Chopra, Rajiv,Cowling, Rebecca,Ellingboe, John W.,Fan, Kristi Y.,Harrison, Boyd L.,Hu, Yun,Jacobsen, Steve,Jennings, Lee D.,Jin, Guixian,Lohse, Peter A.,Malamas, Michael S.,Manas, Eric S.,Moore, William J.,O'Donnell, Mary-Margaret,Olland, Andrea M.,Robichaud, Albert J.,Svenson, Kristine,Wu, JunJun,Wagner, Eric,Bard, Jonathan
, p. 1063 - 1066 (2008/09/19)
Proteolytic cleavage of amyloid precursor protein by β-secretase (BACE-1) and γ-secretase leads to formation of β-amyloid (Aβ) a key component of amyloid plaques, which are considered the hallmark of Alzheimer's disease. Small molecule inhibitors of BACE-1 may reduce levels of Aβ and thus have therapeutic potential for treating Alzheimer's disease. We recently reported the identification of a novel small molecule BACE-1 inhibitor N-[2-(2,5-diphenyl-pyrrol-1-yl)-acetyl]guanidine (3.a.1). We report here the initial hit-to-lead optimization of this hit and the SAR around the aryl groups occupying the S1 and S2′ pockets leading to submicromolar BACE-1 inhibitors.
Studies of the electron-promoted cope cyclization of 2,5-phenyl-substituted 1,5-hexadiene radical anions
Chacko, Silvi A.,Wenthold, Paul G.
, p. 494 - 501 (2007/10/03)
This work describes studies of the electron-promoted Cope cyclization of 2,5-phenyl-1,5-hexadiene radical anions in a flowing afterglow triple quadrupole mass spectrometer. The electronic properties of the hexadienes have been systematically modified by u
One-step preparation of symmetrical 1,4-diketones from α-halo ketones in the presence of Zn-I2 as a condensation agent
Ceylan, Mustafa,Guerdere, M. Burcu,Budak, Yakup,Kazaz, Cavit,Secen, Hasan
, p. 1750 - 1754 (2007/10/03)
Eleven 1,4-diphenylbutane-1,4-diones have been prepared in one step from the corresponding α-halo acetophenones under the action of Zn-I 2 as a condensation agent with moderate to high yields. The mechanistic pathway of the reaction can be explained by the Wurtz-like self-condensation of α-halo ketones. Similarly, 3-chloropentane-2,4-dione gave 3,4-diacetylhexane-2,5-dione, a Wurtz-like condensation product.
Addition von Aldehyden an aktivierte Doppelbindungen, XXIX. Neue Methode zur Darstellung symmetrischer 1,4-Diketone
Stetter, Hermann,Bender, Hans-Juergen
, p. 1226 - 1233 (2007/10/02)
Thiazolium salt-catalysed addition of aliphatic, aromatic, and heterocyclic aldehydes to phenyl vinyl sulfone yields in a three-step addition-elimination mechanism 1,4-diketones (1 - 3) and 1,4-disulfone (23).The analogous reaction with divinyl sulfone leads in good yields to the corresponding 1,4-diketones (1 - 22).
