1590-25-6Relevant academic research and scientific papers
Practical synthesis of acetophenones from phenoltriflates
Garrido, Fabrice,Raeppel, Stéphane,Mann, André,Lautens, Mark
, p. 265 - 266 (2001)
A new practical method for the preparation of acetophenone from aryl triflates is reported. The acyl group is installed by a mixture of SnMe4, Pd(0) and CO (balloon), using a three-component procedure.
Quantitative Design of Bright Fluorophores and AIEgens by the Accurate Prediction of Twisted Intramolecular Charge Transfer (TICT)
Chen, Jie,Chi, Weijie,Jiang, Xiao-Fang,Liu, Wenjuan,Liu, Xiaogang,Lyu, Da,McKechnie, Scott,Qiao, Qinglong,Tan, Davin,Wang, Chao,Xu, Ning,Xu, Zhaochao,Zhang, Qisheng,Zhou, Wei
, p. 10160 - 10172 (2020)
Inhibition of TICT can significantly increase the brightness of fluorescent materials. Accurate prediction of TICT is thus critical for the quantitative design of high-performance fluorophores and AIEgens. TICT of 14 types of popular organic fluorophores
Exploring the Effect of Aliphatic Substituents on Aryl Cyano Amides on Enhancement of Fluorescence upon Binding to Amyloid-β Aggregates
Ehrlich, Rachel S.,Shiao, Alexander L.,Li, Meihan,Teppang, Kristine L.,Jeoung, Kun Yong,Theodorakis, Emmanuel A.,Yang, Jerry
, p. 2946 - 2952 (2021/08/06)
The self-assembly of amyloid-β (Aβ) peptides into amyloid aggregates is a pathological hallmark of Alzheimer's Disease. We previously reported a fluorescent Aryl Cyano Amide (ARCAM) probe that exhibits an increase in fluorescence emission upon binding to Aβ aggregates in solution and in neuronal tissue. Here, we investigate the effect of introducing small aliphatic substituents on the spectroscopic properties of ARCAM both free in solution and when bound to aggregated Aβ. We found that introducing substituents designed to hinder the rotation of bonds between the electron donor and acceptor on these fluorophores can affect the overall brightness of fluorescence emission of the probes in amyloid-free solutions, but the relative fluorescence enhancement of these probes in amyloid-containing solutions is dependent on the location of the substituents on the ARCAM scaffold. We also observed the capability to tune the excitation or emission wavelength of these probes by introducing electron-donating or -withdrawing substituents that putatively affect either the energy required for photoexcitation or the stability of the photoexcited state. These studies reveal new design principles for developing ARCAM-based fluorescent Aβ-binding probes with an enhanced fluorescence signal compared to background and tunable spectroscopic properties, which may lead to improved chemical tools for aiding in the diagnosis of amyloid-associated neurodegenerative diseases.
NOVEL BENZIMIDAZOLE DERIVATIVES
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Paragraph 0252, (2020/01/22)
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Coordination-Induced Stereocontrol over Carbocations: Asymmetric Reductive Deoxygenation of Racemic Tertiary Alcohols
Isomura, Mayuko,Petrone, David A.,Carreira, Erick M.
, p. 4738 - 4748 (2019/03/19)
The inherent difficulty in eliciting facial control over carbocations has limited their utility as intermediates in asymmetric catalysis. We have now shown that a docking strategy involving the reversible coordination of a substrate to a chiral transition-metal catalyst can be used to enable highly stereoselective nucleophilic attack on intermediate tertiary carbocations. This approach has been implemented to achieve the first example of enantioselective reductive deoxygenation of tertiary alcohols. This reduction occurs with high enantio- (up to 96% ee) and regioselectivity (up to >50:1 rr) by applying a novel Hantzsch ester analogue as a convenient hydride source. In-depth mechanistic studies support the involvement of a tertiary carbocation that is coordinated to the iridium metal center via the key allene moiety.
N - heterocyclic compound, intermediate, preparation method, pharmaceutical composition and application (by machine translation)
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, (2017/10/31)
The invention discloses a N - heterocyclic compound, intermediate, preparation method, pharmaceutical composition and application. The invention of SHP2 N - heterocyclic compound to have high selectivity, can effectively inhibit the cell in the SHP2 downstream signal path ERK phosphorylation level, to tumor cells has very good inhibition activity, it has broad drug development prospects; its preparation method is simple, mild reaction conditions, high yield and purity, after treatment is simple, environmental protection, and is favorable for industrial production. (by machine translation)
HEPATITIS C VIRUS INHIBITORS AND USES THEREOF IN PREPARATION OF DRUGS
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, (2017/12/17)
A series of hepatitis C virus (HCV) inhibitors and compositions and applications thereof in the preparation of drugs for treating chronic HCV infection. Especially, a series of compounds that are used as NS5A inhibitors, and compositions and uses thereof in the preparations of drugs.
BIARYL DERIVATIVE AS GPR120 AGONIST
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Paragraph 0306, (2017/11/17)
The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
BINAPHTHYL DERIVATIVE AS ORGANIC SEMICONDUCTOR MATERIAL
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Paragraph 0044, (2017/08/02)
PROBLEM TO BE SOLVED: To provide an organic semiconductor having a relatively simple structure, excellent in stability such as oxidation resistance and solubility to an organic solvent and having processability. SOLUTION: An organic compound contains at least one kind of compound represented by the following chemical formula, where R1 to R4 contain each independently at least one of a hydrogen atom and a halogen atom, a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted alkoxyl group, a substituted or unsubstituted carbonyl group, a substituted or unsubstituted ester group, a substituted or unsubstituted amide group, a substituted or unsubstituted imino group, a substituted or unsubstituted sulfide group, a substituted or unsubstituted sulfoxide group, a substituted or unsubstituted sulfonyl group, a substituted or unsubstituted silyl group, a carboxyl group, a hydroxyl group, a nitro group, a nitrile group, a mercapto group. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
The Multiple Facets of Iodine(III) Compounds in an Unprecedented Catalytic Auto-amination for Chiral Amine Synthesis
Buendia, Julien,Grelier, Gwendal,Darses, Benjamin,Jarvis, Amanda G.,Taran, Frédéric,Dauban, Philippe
supporting information, p. 7530 - 7533 (2016/07/06)
Iodine(III) reagents are used in catalytic one-pot reactions, first as both oxidants and substrates, then as cross-coupling partners, to afford chiral polyfunctionalized amines. The strategy relies on an initial catalytic auto C(sp3)?H amination of the iodine(III) oxidant, which delivers an amine-derived iodine(I) product that is subsequently used in palladium-catalyzed cross-couplings to afford a variety of useful building blocks with high yields and excellent stereoselectivities. This study demonstrates the concept of self-amination of the hypervalent iodine reagents, which increases the value of the aryl moiety.
