4379-54-8Relevant academic research and scientific papers
Direct aerobic carbonylation of C(sp2)-H and C(sp3)-H bonds through Ni/Cu synergistic catalysis with DMF as the carbonyl source
Wu, Xuesong,Zhao, Yan,Ge, Haibo
, p. 4924 - 4927 (2015)
The direct carbonylation of aromatic sp2 and unactivated sp3 C-H bonds of amides was achieved via nickel/copper catalysis under atmospheric O2 with the assistance of a bidentate directing group. The sp2 C-H func
Discovery of disubstituted xylylene derivatives as small molecule direct inhibitors of Keap1-Nrf2 protein-protein interaction
Abed, Dhulfiqar Ali,Hu, Longqin,Lee, Sumi
, (2020/02/13)
The Keap1–Nrf2–ARE system represents a crucial antioxidant defense mechanism that protects cells against reactive oxygen species. Targeting Keap1–Nrf2 protein–protein interaction (PPI) has become a promising drug target for several oxidative stress-relate
Binuclear Pd(I)-Pd(I) Catalysis Assisted by Iodide Ligands for Selective Hydroformylation of Alkenes and Alkynes
Zhang, Yang,Torker, Sebastian,Sigrist, Michel,Bregovi?, Nikola,Dydio, Pawe?
supporting information, p. 18251 - 18265 (2020/11/02)
Since its discovery in 1938, hydroformylation has been thoroughly investigated and broadly applied in industry (>107 metric ton yearly). However, the ability to precisely control its regioselectivity with well-established Rh- or Co-catalysts has thus far proven elusive, thereby limiting access to many synthetically valuable aldehydes. Pd-catalysts represent an appealing alternative, yet their use remains sparse due to undesired side-processes. Here, we report a highly selective and exceptionally active catalyst system that is driven by a novel activation strategy and features a unique Pd(I)-Pd(I) mechanism, involving an iodide-assisted binuclear step to release the product. This method enables β-selective hydroformylation of a large range of alkenes and alkynes, including sensitive starting materials. Its utility is demonstrated in the synthesis of antiobesity drug Rimonabant and anti-HIV agent PNU-32945. In a broader context, the new mechanistic understanding enables the development of other carbonylation reactions of high importance to chemical industry.
SMALL MOLECULE DIRECT INHIBITORS OF KEAP1-NRF2 PROTEIN-PROTEIN INTERACTION
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Paragraph 0095-0096, (2020/07/31)
This patent document diclsoes novel compounds and methods of preventing or treating diseases or conditions related to Keapl-Nrf2 interaction activity by use of the novel compounds. As direct inhibitors of Keapl-Nrf2 interaction, the compounds disclosed herein are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential dmg candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, Parkinson's, and inflammatory bowel disease including ulcerative colitis.
Novel naphthalene based lariat-type crown ethers using direct single electron transfer photochemical strategy
Park, Hea Jung,Sung, Nam Kyung,Kim, Su Rhan,Ahn, So Hyun,Yoon, Ung Chan,Cho, Dae Won,Mariano, Patrick S.
, p. 3681 - 3689 (2014/01/17)
This study explored a direct SET-photochemical strategy to construct a new family of thioene conjugatednaphthalamide fluorophore based lariat-crown ethers which show strong binding properties towards heavy metal ions. Irradiations of designed nitrogen branched (trimethylsilyl)methylthio-terminated polyethylenoxytethered naphthalimides in acidic methanol solutions have led to highly efficient photocyclization reactions to generate naphthalamide based lariat type thiadiazacrown ethers directly in chemo- and regio-selective manners which undergo very facile secondary dehydration reactions during separation processes to produce their corresponding amidoenethio ether cyclic products tethered with electron donating diethyleneoxy- and diethyenethio-side arm chains. Fluorescence and metal cation binding properties of the lariat type enamidothio products were examined. The photocyclized amidoenethio products, thioene conjugated naphthalamide fluorophore containing lariat-thiadiazacrowns exhibited strong fluorescence emissions in region of 330-450 nm along with intramolecular exciplex emissions in region of 450-560 nm with their maxima at 508 nm. Divalent cation Hg2+ and Pb2+ showed strong binding to sulfur atom(s) in side arm chain and atoms in enethiadiazacrown ether rings which led to significant enhancement of fluorescence from its chromophore singlet excited state and concomitant quenching of exciplex emission. The dual fluorescence emission responses towards divalent cations might.
Catalytic Friedel-Crafts reaction of aminocyclopropanes
De Nanteuil, Florian,Loup, Joachim,Waser, Jeroime
supporting information, p. 3738 - 3741 (2013/08/15)
A Lewis acid catalyzed Friedel-Crafts reaction between donor-acceptor aminocyclopropanes and indoles and other electron-rich aromatic compounds is reported. Indole alkylation at the C3 position was generally obtained for a broad range of functional groups and substitution patterns. In the case of C3-substituted indoles, C2 alkylation was observed. The reaction gives a rapid access to gamma amino acid derivatives present in numerous bioactive molecules.
PHOTOCYCLIZATION OF N-(DIALKYLAMINOALKYL) AROMATIC 1,2-DICARBOXIMIDES. X-RAY MOLECULAR STRUCTURE OF A STEREOISOMER OF 4-BENZYL-2-HYDROXY-3-PHENYL-4,6-DIAZATRICYCLO2.6>DODECA-1(12),8,10-TRIEN-7-ONE
Coyle, John D.,Smart Lesley E.,Challiner, John F.,Haws, Edmud J.
, p. 121 - 130 (2007/10/02)
U.v. irradiation of Mannich bases derived from chloro- or methoxycarbonyl (but not nitro)- substituted phthalimides, pyridinedicarboximides, or naphthalene-2,3-dicarboximide gives rise to products with a new imidazolidine ring.Substrates from unsymmetrical imides lead preferentially (though not exclusively) to one orientation of reaction.Two diastereoisomeric products are often formed, and the relative stereochemistry can be assigned on the basis of n.m.r. data; in one case the stereochemistry is confirmed by X-ray crystallographic analysis.The two diastereoisomers are, under certain conditions, interconverted photochemically.
