574741-55-2Relevant academic research and scientific papers
COMPOSITIONS AND METHODS FOR PROTEIN LABELING, MODIFICATION, ANALYSIS, AND TARGETED DELIVERY
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Paragraph 00226; 00228, (2020/01/24)
The invention relates to chemically reactive and/or biologically active compounds, reagents and compositions thereof. More particularly, the invention provides novel reagents that are useful in chemical synthesis, functionalization, delivery, probing and/or analytical measurements of small molecule drugs, proteins, antibodies and other biomolecules. The invention provides novel biologically active agents useful as diagnostics or therapeutics, and related composition and methods of uses thereof.
Electrochemistry-Enabled Ir-Catalyzed Vinylic C-H Functionalization
Yang, Qi-Liang,Xing, Yi-Kang,Wang, Xiang-Yang,Ma, Hong-Xing,Weng, Xin-Jun,Yang, Xiang,Guo, Hai-Ming,Mei, Tian-Sheng
supporting information, p. 18970 - 18976 (2019/12/04)
Synergistic use of electrochemistry and organometallic catalysis has emerged as a powerful tool for site-selective C-H functionalization, yet this type of transformation has thus far mainly been limited to arene C-H functionalization. Herein, we report the development of electrochemical vinylic C-H functionalization of acrylic acids with alkynes. In this reaction an iridium catalyst enables C-H/O-H functionalization for alkyne annulation, affording α-pyrones with good to excellent yields in an undivided cell. Preliminary mechanistic studies show that anodic oxidation is crucial for releasing the product and regeneration of an Ir(III) intermediate from a diene-Ir(I) complex, which is a coordinatively saturated, 18-electron complex. Importantly, common chemical oxidants such as Ag(I) or Cu(II) did not give significant amounts of the desired product in the absence of electrical current under otherwise identical conditions.
Parallel Kinetic Resolution of Intramolecular Furan Diels-Alder Cycloadducts via Asymmetric Hydroboration
Fulgheri, Tamara,Cornwall, Philip,Turner, Andrew R.,Sweeney, Joseph B.,Gill, Duncan M.
supporting information, p. 7223 - 7227 (2019/11/19)
We report parallel kinetic resolution of intramolecular Diels-Alder cycloadducts, where up to five stereocentres are defined using asymmetric hydroboration as the enantiodiscriminating reaction, and reveal evidence for dynamic kinetic resolution based on a reversible cycloaddition.
Polymerizable polar compound, liquid crystal composition, and liquid crystal display element
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Paragraph 0459; 0460; 0511; 0515; 0516, (2017/09/08)
Provided is a polar compound having high chemical stability, high ability to align liquid crystal molecules, and high solubility in a liquid crystal composition, and which has a large voltage holding ratio when used in a liquid crystal display element. A
Cyclization cascades via N -amidyl radicals toward highly functionalized heterocyclic scaffolds
Fuentes, Noelia,Kong, Wangqing,Fernández-Sánchez, Luis,Merino, Estíbaliz,Nevado, Cristina
supporting information, p. 964 - 973 (2015/01/30)
The addition of a variety of radicals to the double bond of N-(arylsulfonyl)acrylamides can trigger cyclization/aryl migration/desulfonylation cascades via amidyl radical intermediates 2. Herein, we demonstrate the synthetic utility of these intermediates in subsequent C-C and C-X bond-forming events to rapidly build up molecular complexity. First, we describe a regioselective one-pot synthesis of CF3-, SCF3-, Ph2(O)P-, and N3-containing indolo[2,1-a]isoquinolin-6(5H)-ones from N-[(2-ethynyl)arylsulfonyl]acrylamides through a multi-step radical reaction cascade. The process involves the one-pot formation of four new bonds (one C-X, two C-C, and one C-N), a formal 1,4-aryl migration, and desulfonylation of the starting material. Second, we present a one-pot synthesis of 3,3-disubstituted-2-dihydropyridinones from N-(arylsulfonyl)acrylamides and 1,3-dicarbonyl compounds. In this case, a silver-catalyzed radical cascade process involving the sequential formation of two new C-C bonds and one C-N bond, a formal 1,4-aryl migration, and desulfonylation of the starting material explains the regioselective formation of densely functionalized heterocycles in a straightforward manner. Control experiments have unraveled the key intermediates as well as the sequence of individual steps involved in these transformations.
Synthesis of Denosomin-Vitamin D3 Hybrids and Evaluation of Their Anti-Alzheimer's Disease Activities
Sugimoto, Kenji,Yajima, Hisanari,Hayashi, Yusuke,Minato, Daishiro,Terasaki, Sayuri,Tohda, Chihiro,Matsuya, Yuji
supporting information, p. 5910 - 5913 (2015/12/11)
As an extension of previously conducted studies on developing an anti-Alzheimer's disease agent, denosomin (1-deoxy-24-norsominone, an artificial inducer of neurite elongation), derivatives were designed and synthesized based on the hypothesis that our denosomin would exhibit axonal extension activity via a 1,25D3-membrane-associated, rapid response steroid-binding protein (1,25D3-MARRS) pathway. The biological assay revealed that the hybridization of characteristic δ-lactone in denosomin and the triene moiety in VD3 was effective to enhance the nerve re-extension activity in amyloid β (Aβ)-damaged neurons.
Ruthenium- and rhodium-catalyzed cross-coupling reaction of acrylamides with alkenes: Efficient access to (Z,E)-dienamides
Zhang, Jian,Loh, Teck-Peng
supporting information, p. 11232 - 11234 (2013/01/15)
Ruthenium- and rhodium-catalyzed direct oxidative cross-coupling reactions of acrylamides with alkenes were developed. These methods provide an efficient route for the synthesis of (Z,E)-dienamides in excellent yields with good stereoselectivity. The catalytic systems allowed oxidative olefination of a wide range of alkenes bearing different functional groups, such as CO2R, COMe, SO2Ph, aryl, CONHBn, CN, PO(OEt)2, as well as Weinreb amide.
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND PHARMACEUTICAL APPLICATION THEREOF
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Page/Page column 185, (2010/11/26)
It is intended to provide a compound represented by the general formula (I): (I) (wherein all the symbols are as defined in the description) which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.
