4703-15-5Relevant academic research and scientific papers
Ligand-Controlled Regiodivergence for Catalytic Stereoselective Semireduction of Allenamides
Hajiloo Shayegan, Mojtaba,Li, Zhong-Yuan,Cui, Xin
supporting information, (2021/12/02)
Ligand-controlled regiodivergence has been developed for catalytic semireduction of allenamides with excellent chemo- and stereocontrol. This system also provides an example of catalytic regiodivergent semireduction of allenes for the first time. The divergence of the semireduction is enabled by ligand switch with the same palladium pre-catalyst under operationally simple and mild conditions. Monodentate ligand XPhos exclusively promotes selective 1,2-semireduction to afford allylic amides, while bidentate ligand BINAP completely switched the regioselectivity to 2,3-semireduction, producing (E)-enamide derivatives.
PLASMA KALLIKREIN INHIBITORS AND USES THEREOF
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Paragraph 0731; 0732, (2021/03/19)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
Conformational control of bis-urea self-assembled supramolecular pH switchable low-molecular-weight hydrogelators
Chippindale, Ann M.,Christie, William,Gavriel, Alexander G.,German, Ian M.,Hayes, Wayne,O'Donnell, Adam D.
, (2021/11/03)
We report the synthesis and investigation into the structure-property relationships of eight different low molecular weight hydrogelators based on a bisaromatic urea core unit, all of which form gels as the pH of the solution is lowered. The low molecular weight hydrogelators are functionalized with carboxylic acid moieties on one aromatic ring, and the other aromatic ring features a nitro functional group either in the meta- or paraposition relative to the urea linkage. Ortho-methyl substituents were installed on the aromatic rings to enforce a non-coplanar arrangement between the phenyl and urea moieties. Gel formation was triggered by the addition of a mineral acid or the ring-opening hydrolysis of glucono-δ-lactone. The low molecular weight hydrogelators were studied by a variety of analytical techniques, including NMR spectroscopy and rheology. In addition, their ability to uptake a dye, methylene blue, was determined by UV-vis spectroscopy. (Figure Presented)
Self-Immolative System for Disclosure of Reactive Electrophilic Alkylating Agents: Understanding the Role of the Reporter Group
Chippindale, Ann M.,Gavriel, Alexander G.,Hayes, Wayne,Khurana, Gurjeet S.,Leroux, Flavien,Lewis, Viliyana G.,Russell, Andrew T.,Sambrook, Mark R.
, p. 10263 - 10279 (2021/08/16)
The development of stable, efficient chemoselective self-immolative systems, for use in applications such as sensors, requires the optimization of the reactivity and degradation characteristics of the self-immolative unit. In this paper, we describe the effect that the structure of the reporter group has upon the self-immolative efficacy of a prototype system designed for the disclosure of electrophilic alkylating agents. The amine of the reporter group (a nitroaniline unit) was a constituent part of a carbamate that functioned as the self-immolative unit. The number and position of substituents on the nitroaniline unit were found to play a key role in the rate of self-immolative degradation and release of the reporter group. The position of the nitro substituent (meta- vs para-) and the methyl groups in the ortho-position relative to the carbamate exhibited an influence on the rate of elimination and stability of the self-immolative system. The ortho-methyl substituents imparted a twist on the N-C (aromatic) bond leading to increased resonance of the amine nitrogen's lone pair into the carbonyl moiety and a decrease of the leaving character of the carbamate group; concomitantly, this may also make it a less electron-withdrawing group and lead to less acidification of the eliminated β-hydrogen.
Three-Component Ring-Opening Reactions of Cyclic Ethers, α-Diazo Esters, and Weak Nucleophiles under Metal-Free Conditions
Lu, Lin,Chen, Chuwei,Jiang, Huanfeng,Yin, Biaolin
, p. 14385 - 14395 (2018/11/27)
A protocol for three-component reactions of cyclic ethers, α-diazo esters, and weak nitrogen, oxygen, carbon, and sulfur nucleophiles (pKa = 2.2-14.8) to afford a variety of structurally complex α-oxyalkylated esters is reported. These reactions involve intermolecular activation of the cyclic ether (present in excess) by the α-diazo ester to form an oxonium ylide under metal-free conditions, followed by ring opening by the nucleophile.
Method and using tracer charged ion channel
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Paragraph 0422; 0424; 0425-0427, (2018/08/20)
The invention provides compounds, compositions, methods, and kits for the treatment of pain, itch, and neurogenic inflammation.
Development of 2, 4-diaminoquinazoline derivatives as potent PAK4 inhibitors by the core refinement strategy
Hao, Chenzhou,Huang, Wanxu,Li, Xiaodong,Guo, Jing,Chen, Meng,Yan, Zizheng,Wang, Kai,Jiang, Xiaolin,Song, Shuai,Wang, Jian,Zhao, Dongmei,Li, Feng,Cheng, Maosheng
, p. 1 - 13 (2017/03/16)
Upon analysis of the reported crystal structure of PAK4 inhibitor KY04031 (PAK4 IC50?=?0.790?μM) in the active site of PAK4, we investigated the possibility of changing the triazine core of KY04031 to a quinazoline. Using KY04031 as a starting
NOVEL KCNQ POTASSIUM CHANNEL AGONIST, AND PREPARATION METHOD THEREFOR AND USE THEREOF
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Paragraph 0040; 0041, (2017/03/21)
The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, conv
Enhancing the Gas Permeability of Tr?ger's Base Derived Polyimides of Intrinsic Microporosity
Lee, Michael,Bezzu, C. Grazia,Carta, Mariolino,Bernardo, Paola,Clarizia, Gabriele,Jansen, Johannes C.,McKeown, Neil B.
, p. 4147 - 4154 (2016/07/06)
A series of four novel Tr?ger's base (TB) derived polyimides of intrinsic microporosity (PIM-TB-PI) is reported. The TB diamine monomer (4MTBDA) possesses four methyl groups in order to restrict rotation about the C-N imide bonds in the resulting polymers
Nickel-catalyzed monoarylation of ammonia
Borzenko, Andrey,Rotta-Loria, Nicolas L.,Macqueen, Preston M.,Lavoie, Christopher M.,McDonald, Robert,Stradiotto, Mark
, p. 3773 - 3777 (2015/03/18)
Structurally diverse (hetero)aryl chloride, bromide, and tosylate electrophiles were employed in the Ni-catalyzed monoarylation of ammonia, including chemoselective transformations. The employed JosiPhos/[Ni(cod)2] catalyst system enables the use of commercially available stock solutions of ammonia, or the use of ammonia gas in these reactions, thereby demonstrating the versatility and potential scalability of the reported protocol. Proof-of-principle experiments established that air-stable [(JosiPhos)NiCl2] precatalysts can be employed successfully in such transformations. Lighten Up: The substrate scope of the title reaction includes (hetero)aryl chloride, bromide, and tosylate electrophiles. The versatility and potential scalability of the reported method is demonstrated by the use of either commercially available stock solutions of ammonia or ammonia gas.
