112632-96-9Relevant articles and documents
Design, Synthesis, and Anticancer Activity of Novel Benzothiazole Analogues
Hassan, Aisha Y.,Sarg, Marwa T.,Hussein, Ebtehal M.
, p. 1437 - 1457 (2019)
On the pharmaceutical account of the reported anticancer activity of benzothiazole derivatives, differently substituted benzothiazole derivatives 2a–c to 34a,b, attached at 2-position to different heterocyclic moieties, were synthesized via different chemical reactions. Thirteen of the newly synthesized compounds were selected by the National Cancer Institute, Bethesda, Maryland, USA, and evaluated for their in vitro antitumor activity against 60 human tumor cell lines in a one-dose screening panel among which two compounds 4 and 17 showed high activity and were selected for further evaluation in the five-dose full panel assay, in which compound 4 exerted powerful growth inhibitory activity against all cell lines with GI50 ranging from 0.683 to 4.66?μM/L in addition to excellent lethal activity against most of the cell lines.
Excimers beyond pyrene: A far-red optical proximity reporter and its application to the label-free detection of DNA
Han, Garam,Kim, Dongwook,Park, Younbong,Bouffard, Jean,Kim, Youngmi
, p. 3912 - 3916 (2015)
A family of organic chromophores that, like pyrene, forms emissive excimers is reported. Their chemical and photophysical properties are superior to pyrene for the design of chemo- and biosensors. Unlike hydrophobic pyrene, which requires excitation by cell-damaging UV irradiation, these polar dyes absorb strongly in the visible range, and their excimers emit brightly in the red to far-red region of the electromagnetic spectrum. The intensity of the emission signal is greatly increased upon formation of a preassociated dimer that is triggered upon aggregation or crystallization. In demonstration of the potential of this new family of excimer-forming dyes, a probe that is capable of detecting label-free DNA in water down to 10 pM and also doubles as a visualization agent for DNA in gel electrophoresis is reported.
Alkene-modified Fe3O4 nanoparticle-mediated construction of functionalized mesoporous poly(ionic liquid)s: Synergistic catalysis of mesoporous confinement effect and hydrogen proton for organic transformations
Liu, Zhong-Qiu,Li, Sheng-Nan,Zeng, Qing-Shuai,Liu, Yu-Jing,You, Jin-Mao,Ying, An-Guo
, (2021/02/21)
The preparation of mesoporous poly(ionic liquid)s (MPILs) is critically fundamental for the design of heterogeneous catalysts, whereas traditional methods are difficult to obtain these materials with both well-defined mesoporous structure and unique functionality. Here, HClO4-functionalized MPILs with well-defined mesoporous structure were successfully fabricated, in which the alkene-modified Fe3O4 nanoparticles as structural reinforcer play a vital role for mesoporous structure formation. The MPILs were characterized by N2 adsorption/desorption, scanning electron microscope (SEM), transmission Electron Microscope (TEM), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), thermogravimetric analysis (TGA), and vibration sample magnetometry (VSM), and the results confirm that MPILs possess moderate surface area, well-defined mesoporosity, abundant active ionic centers, as well as efficient magnetic recovery. The resulting MPILs show excellent catalytic activity for condensation reaction and Knoevenagel condensation. The kinetic study reveals that the excellent catalytic activity of MPILs is attributed to the synergistic catalysis of mesoporous confinement effect and hydrogen proton from MPILs, albeit with mass transfer resistance produced by mesoporous channels. Further, the catalyst can be recovered using an external magnetic field and reused at least 10 times without a considerable decrease in its catalytic activity. Finally, alkene-modified Fe3O4 nanoparticle-mediated mesoporous construction promotes a textural engineering approach to the development of novel mesoporous materials for other applications.
A process for preparing two aromatic ring substituted olefins method
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Paragraph 0046-0048, (2017/06/08)
The invention relates to an efficient environment-friendly catalyst, and a new method for preparing double-(hetero)aromatic-ring substituted alkene under a room-temperature condition by taking water as a reaction medium. The method comprises: taking n-propylamine supported by super-paramagnetism nanometer particles and modified by ion atmosphere as a catalyst, and under the conditions of room temperature, normal pressure and water reaction medium, performing Knoevenagel condensation reaction on an (hetero)aromatic-ring substituted active alkene substance and an aromatic aldehyde, so as to obtain a corresponding double-(hetero)aromatic-ring substituted alkene derivative. The reaction yield is not obviously reduced after the supported catalyst is repeatedly used for 8 times. The method is simple in operation, high in yield, simple in catalyst recovery, good in reusability of the catalytic reaction system and mild in reaction conditions, and has good industrialization prospect.
Simple, efficient, and green method for synthesis of trisubstituted electrophilic alkenes using lipase as a biocatalyst
Borse, Bhushan Nanasaheb,Shukla, Sanjeev Ramchandra,Sonawane, Yogesh Ashok
experimental part, p. 412 - 423 (2011/11/12)
A simple and efficient Knoevenagel condensation method for the synthesis of trisubstituted electrophilic alkenes was developed using lipase as a biocatalyst. Knoevenagel condensation was performed using the conventional method and using lipases (Aspergillus oryzae or Rhizopus oryzae) as biocatalysts, and reaction time, reaction temperature, yield, and recyclability were compared. Using a lipase as a biocatalyst eliminated the need for bases such as piperidine and pyridine. A wide range of aromatic aldehydes and ketones readily undergo condensation with active methylene compounds. The workup procedure is also very simple, and yields of the reactions are in the range of 75%to 95%. Both the biocatalysts were effectively recycled four times with no major decrease in the yield of product. The remarkable catalytic activity and reusability of lipase widens its applicability in Knoevenagel condensation with good to excellent yields for synthesis of trisubstituted electrophilic alkenes.Copyright Taylor & Francis Group, LLC.
A splendid method for synthesis of 2-(benzothiazole)-3-phenyl acrylonitrile derivatives catalysed by piperdine
Maddila, Suresh,Jonnalagadda, Sreekanth B.
, p. 467 - 471 (2012/10/29)
A simple and efficient method is developed for the synthesis of 2-(benzothiazol-2-yl)-3- (substituted phenyl)acrylonitrile from 2-(benzothiazole-2-yl)-3-oxopentanedinitrile and aromatic aldehydes in the presence of a catalytic amount of piperdine into ethanol at reflux. Advantage of this procedure is relatively good yields (81-86%) with short reaction times (1.5-3 h), under moderate reaction conditions and simple workup procedure, plus easy preparation and handling of the catalyst.
A basic ionic liquid catalyzed reaction of benzothiazole, aldehydes, and 5,5-dimethyl-1,3-cyclohexanedione: Efficient synthesis of tetrahydrobenzo[b] pyrans
Wen, Li-Rong,Xie, Huai-Yuan,Li, Ming
scheme or table, p. 954 - 959 (2009/12/05)
(Chemical Equation Presented) A fast, mild, and quantitative procedure for the preparation of tetrahydrobenzo[b]pyran derivatives in the presence of an easily accessible basic ionic liquid - [bmIm]OH(3-butyl-1- methylimidazoliumhydroxide) as the catalyst
UNCATALYZED KNOEVENAGEL CONDENSATION OF 2-CYANOMETHYLBENZOTHIAZOLE WITH AROMATIC ALDEHYDES. PREPARATION OF 3-ARYL-2-(2-BENZOTHIAZOLYL)-ACRYLONITRILES AND 3-(2-BENZOTHIAZOLYL)-COUMARIN IMINES
Dryanska, Veneta
, p. 325 - 329 (2007/10/02)
A series of 3-aryl-2-(2-benzothiazolyl)-acrylonitriles (3a-n) and 3-(2-benzothiazolyl)-coumarin imines (5a-f) are prepared in good to high yields by refluxing solutions of 2-cyanomethylbenzothiazole (1) and aromatic aldehydes (2, 4) in ethanol. Key words:
