94112-58-0Relevant articles and documents
Shuttle arylation by Rh(I) catalyzed reversible carbon–carbon bond activation of unstrained alcohols
Lutz, Marius D.R.,Gasser, Valentina C.M.,Morandi, Bill
supporting information, p. 1108 - 1119 (2021/04/19)
The advent of transfer hydrogenation and borrowing hydrogen reactions paved the way to manipulate simple alcohols in previously unthinkable manners and circumvented the need for hydrogen gas. Analogously, transfer hydrocarbylation could greatly increase the versatility of tertiary alcohols. However, this reaction remains unexplored because of the challenges associated with the catalytic cleavage of unactivated C–C bonds. Herein, we report a rhodium(I)-catalyzed shuttle arylation cleaving the C(sp2)–C(sp3) bond in unstrained triaryl alcohols via a redox-neutral β-carbon elimination mechanism. A selective transfer hydrocarbylation of substituted (hetero)aryl groups from tertiary alcohols to ketones was realized, employing benign alcohols as latent C-nucleophiles. All preliminary mechanistic experiments support a reversible β-carbon elimination/migratory insertion mechanism. In a broader context, this novel reactivity offers a new platform for the manipulation of tertiary alcohols in catalysis.
NHC-coordinated palladacycle catalyzed 1,2-addition of arylboronates to unactivated ketones
Akiyama, Ryo,Sugaya, Mariko,Shinozaki, Hiraku,Yamamoto, Tetsuya
, p. 1193 - 1201 (2019/05/06)
Palladium catalyzed intermolecular 1,2-addition of arylboronate to unactivated ketone was investigated. NHC-coordinated palladacycle 4c exhibited catalytic activity for the reactions and provided the corresponding tertiary alcohols and γ,γ-disubstituted γ-lactones in good to excellent yields.
Optimization of TRPV6 calcium channel inhibitors using a 3D ligand-based virtual screening method
Simonin, Céline,Awale, Mahendra,Brand, Michael,Van Deursen, Ruud,Schwartz, Julian,Fine, Michael,Kovacs, Gergely,H?fliger, Pascal,Gyimesi, Gergely,Sithampari, Abilashan,Charles, Roch-Philippe,Hediger, Matthias A.,Reymond, Jean-Louis
supporting information, p. 14748 - 14752 (2016/02/05)
Herein, we report the discovery of the first potent and selective inhibitor of TRPV6, a calcium channel overexpressed in breast and prostate cancer, and its use to test the effect of blocking TRPV6-mediated Ca2+-influx on cell growth. The inhib