39998-25-9Relevant articles and documents
7-azabenzofuran derivatives and application thereof in antitumor drugs
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Paragraph 0031-0033, (2021/01/29)
The invention discloses a 7-azabenzofuran compound with anti-tumor activity and a synthesis method of the 7-azabenzofuran compound. The key synthesis step is that pyridine oxynitride is used as a substrate and reacts with acyl chloride to generate the 7-azabenzofuran derivative. An anti-tumor activity test proves that the 7-azabenzofuran derivative provided by the invention has strong anti-tumor activity on various tumor cells, including human leukemia cells K562, human hepatoma carcinoma cells HepG2 and human colon cancer cells HCT116, and is expected to be developed into a new anti-tumor drug.
Photocatalytic Hydromethylation and Hydroalkylation of Olefins Enabled by Titanium Dioxide Mediated Decarboxylation
Zhu, Qilei,Nocera, Daniel G.
supporting information, p. 17913 - 17918 (2020/12/04)
A versatile method for the hydromethylation and hydroalkylation of alkenes at room temperature is achieved by using the photooxidative redox capacity of the valence band of anatase titanium dioxide (TiO2). Mechanistic studies support a radical-based mechanism involving the photoexcitation of TiO2 with 390 nm light in the presence of acetic acid and other carboxylic acids to generate methyl and alkyl radicals, respectively, without the need for stoichiometric base. This protocol is accepting of a broad scope of alkene and carboxylic acids, including challenging ones that produce highly reactive primary alkyl radicals and those containing functional groups that are susceptible to nucleophilic substitution such as alkyl halides. This methodology highlights the utility of using heterogeneous semiconductor photocatalysts such as TiO2 for promoting challenging organic syntheses that rely on highly reactive intermediates.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH APJ RECEPTOR ACTIVITY
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Page/Page column 146, (2019/09/18)
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol "APLNR"). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.
Dynamic Combinatorial Chemistry to Identify Binders of ThiT, an S-Component of the Energy-Coupling Factor Transporter for Thiamine
Monjas, Leticia,Swier, Lotteke J. Y. M.,Setyawati, Inda,Slotboom, Dirk J.,Hirsch, Anna K. H.
supporting information, p. 1693 - 1696 (2017/10/27)
We applied dynamic combinatorial chemistry (DCC) to identify ligands of ThiT, the S-component of the energy-coupling factor (ECF) transporter for thiamine in Lactococcus lactis. We used a pre-equilibrated dynamic combinatorial library (DCL) and saturation-transfer difference (STD) NMR spectroscopy to identify ligands of ThiT. This is the first report in which DCC is used for fragment growing to an ill-defined pocket, and one of the first reports for its application with an integral membrane protein as target.
PROCESS FOR PREPARING BISPHENOL
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Page/Page column 26, (2011/12/12)
Provided is a process for producing a bisphenol compound stably at a high conversion and with high selectivity over a long period. A process for producing a bisphenol compound by feeding a phenol compound and a carbonyl compound continuously to a reactor packed with an acid catalyst, characterized in that the acid catalyst is a sulfonic-acid-form cation-exchange resin in which part of the sulfo groups have been modified with at least any one of 2-pyridylalkanethiol compounds and 3-pyridylalkanethiol compounds.
Chemoselective photochemical surface reaction - Ketene versus carbene reactivity from the photolysis of saturated monolayers of pyridyl diazoesters on single-crystal Pt
Pitters, Jason L.,Adkinson, Dana K.,Griffiths, Keith,Norton, Peter R.,Workentin, Mark S.
, p. 117 - 121 (2011/04/23)
Irradiation of saturated monolayers of 3-and 4-substituted pyridyl diazoacetates on single-crystal Pt surfaces leads to either the corresponding reactive carbene or stable ketene intermediate with the chemoselectivity determined by the position of the photoreactive substituent on the pyridyl ring, which ultimately directs the available interactions with neighboring substrates.
Design, synthesis, and evaluation of inhibitors for severe acute respiratory syndrome 3C-like protease based on phthalhydrazide ketones or heteroaromatic esters
Zhang, Jianmin,Pettersson, Hanna I.,Huitema, Carly,Niu, Chunying,Yin, Jiang,James, Michael N. G.,Eltis, Lindsay D.,Vederas, John C.
, p. 1850 - 1864 (2008/02/02)
The 3C-like protease (3CLpro), which controls the severe acute respiratory syndrome (SARS) coronavirus replication, has been identified as a potential target for drug design in the treatment of SARS. A series of tetrapeptide phthalhydrazide ketones, pyridinyl esters, and their analogs have been designed, synthesized, and evaluated as potential SARS 3CLpro inhibitors. Some pyridinyl esters are identified as very potent inhibitors, with IC50 values in the nanomolar range (50-65 nM). Electrospray mass spectrometry indicates a mechanism involving acylation of the active site cysteine thiol for this class of inhibitors.
Hydration of pyridylketenes: Formation of acid enol and dihydropyridine (Eneaminone) transients
Allen, Annette D.,Fedorov, Andrei V.,Tidwell, Thomas T.,Vukovic, Sinisa
, p. 15777 - 15783 (2007/10/03)
2-, 3-, and 4-Pyridylketenes 4 formed in water by photochemical Wolff rearrangements using flash photolysis undergo rapid hydration forming transient intermediates observed by UV spectroscopy. 3-Pyridylketene (3-4) formed the acid enol intermediate 3-10 which was converted to the acid 3-11, and phenylketene gave similar behavior. 4-Pyridylketene (4-4) reacted with a similar initial rate constant of 5.0 × 104 s-1 for decay of an absorption at 275 nm, with concomitant formation of a strong absorption at 370 nm with the same rate constant. The intermediate absorbing at 370 nm decayed with a lifetime 2.4 × 103 fold longer than that of the ketene, and is identified as 4-(carboxymethylene)-1,4-dihydropyridine (4-13), resulting from conjugate 1,6-addition of H2O to 4-4. 2-Pyridylketene (2-4) underwent hydration with a similar rate constant of 1.1 × 104 s-1 forming a transient with a UV absorption with maxima at 310 and 380 nm that decayed with biexponetial kinetics, with rate constants slower than the rate of formation by factors of 5.2 and 110, respectively. These results are interpreted as indicating the presence of two species, namely Z- and E-2-(carboxymethylene)-1,2-dihydropyridines (2-13), resulting from conjugate 1,4-addition of H2O to 2-4. The identifications of the 1,2- and 1,4-(carboxymethylene)dihydropyridines 2- and 4-13 were confirmed by comparison of their UV spectra with those of the corresponding N-methyl derivatives. The amination of 2-pyridylketene in CH3CN was reinvestigated, and spectroscopic evidence, computational studies, and preparation of the N-methyl analogue demonstrated formation of the 1,2-dihydropyridine Z-2-8f as the long-lived intermediate.
Efficient Syntheses of Acromelic Acids B and E, Which Are Potent Neuroexcitatory Amino Acids
Horikawa, Manabu,Hashimoto, Kimiko,Shirahama, Haruhisa
, p. 331 - 334 (2007/10/02)
(-)-Acromelic acid B (2) was synthesized from 2-cyano-3-(2-hydroxyethyl)pyridine (4) in 21percent overall yield.Acromelic acid E (3) was also prepared on the way of above synthesis.
Heterocyclic Amplifiers of Phleomycin. VIII Mono- and Bis-(5'-substituted 1',3',4'-thiadiazol-2'-yl)pyridines and Mono(5'-substituted 1',3',4'-thiadiazol-2'-ylmethyl)pyridines
Barlin, Gordon B.
, p. 1491 - 1497 (2007/10/02)
A series of mono- and bis-(5'-substituted 1',3',4'-thiadiazol-2'-yl)pyridines with strongly basic side chains, e.g., 3,5-bispyridine (1), and (5'-substituted 1',3',4'-thiadiazol-2'-ylmethyl)pyridines have been prepared for evaluation as amplifiers of phleomycin.Five of this six bis(5'-substituted 1',3',4'-thiadiazol-2'-yl)pyridines were themselves antibacterial under the test conditions, but compounds (1) and the mono (5'-substituted 1',3',4'-thiadiazol-2'-yl)-pyridines and -methylpyridines displayed moderate two-to-three-star activity.
