26214-65-3Relevant academic research and scientific papers
Rational Development of Novel Activity Probes for the Analysis of Human Cytochromes P450
Sellars, Jonathan D.,Skipsey, Mark,Sadr-ul-Shaheed,Gravell, Sebastian,Abumansour, Hamza,Kashtl, Ghasaq,Irfan, Jawaria,Khot, Mohamed,Pors, Klaus,Patterson, Laurence H.,Sutton, Chris W.
, p. 1122 - 1128 (2016)
The identification and quantification of functional cytochromes P450 (CYPs) in biological samples is proving important for robust analyses of drug efficacy and metabolic disposition. In this study, a novel CYP activity-based probe was rationally designed and synthesised, demonstrating selective binding of CYP isoforms. The dependence of probe binding upon the presence of NADPH permits the selective detection of functionally active CYP. This allows the detection and analysis of these enzymes using biochemical and proteomic methodologies and approaches.
Synthesis and Configurations of (-)-Furospongin-1 and (+)-Dihydrofurospongin-2
Tan, Dong-Xing,Xu, Ze-Jun,Chen, Hui-Jun,Wu, Yikang,You, Jun
, p. 946 - 957 (2016)
The long-known furanoterpenes furospongin-1 and dihydrofurospongin-2 were synthesized for the first time using a chiral-pool-based route in an effort to secure the previous configurational assignments. The key C-11 stereogenic centre was taken from D-mannose, and the C-13 alkyl centre was installed exploiting the chirality of mannose. Due to deprotonation and/or enolization of the building blocks used, introduction of the furan moieties was problematic, and so some reactions had to be avoided. The trisubstituted alkene was most satisfactorily constructed using a Julia-Kocienski olefination in 1,2-dimethoxyethane, with the best (E)/(Z) ratio achieved using a secondary sulfone. The synthetic samples not only provided the first unequivocal piece of evidence for the C-13 configuration of both natural products, but also confirmed the absolute configuration at C-11 of furospongin-1.
A new two-dimensional donor/acceptor copolymer based on 4,8-bis(2′-ethylhexylthiophene)thieno[2,3-f]benzofuran for high-performance polymer solar cells
Fan, Ling,Cui, Ruili,Guo, Xiuping,Qian, Dong,Qiu, Beibei,Yuan, Jun,Li, Yongfang,Huang, Wenlong,Yang, Junliang,Liu, Weifang,Xu, Xinjun,Li, Lidong,Zou, Yingping
, p. 5651 - 5659 (2014)
A new alkylthienyl substituted thieno[2,3-f]benzofuran (TBF)-based polymer (PTBFTDTBT) was synthesized and characterized. PTBFTDTBT had a high molecular weight, good solubility in common organic solvents, broad visible absorption from 300 to 750 nm, and a relatively deep highest occupied molecular orbital level (-5.2 eV). PTBFTDTBT also showed a field hole mobility up to the order of 10-2 using an organic field effect transistor (OFET) method and an order of 10-2 using a space-charge-limited current (SCLC) method. With the structure of indium tin oxide (ITO)/poly(3,4-ethylenedioxythiophene): polystyrene sulfonate/PTBFTDTBT:PC71BM (1:2, w/w)/Ca/Al, a power conversion efficiency of 6.42% was obtained with a high short circuit current (Jsc) of 13.51 mA cm-2 and fill factor (FF) of 61%, under the illumination of AM1.5G, at 100 mW cm-2, without any post-treatment. The study demonstrates that TBF is a promising building block for organic electronics. This journal is the Partner Organisations 2014.
Directed metalation cascade to access highly functionalized thieno[2,3-f ]benzofuran and exploration as building blocks for organic electronics
Aeschi, Yves,Li, Hui,Cao, Zhencai,Chen, Songjie,Amacher, Anneliese,Bieri, Nathalie,Oezen, Bilal,Hauser, Juerg,Decurtins, Silvio,Tan, Songting,Liu, Shi-Xia
, p. 5586 - 5589 (2013)
A tandem directed metalation has been successfully applied to the preparation of thieno[2,3-f]benzofuran-4,8-dione, providing an efficient and facile approach to symmetrically and unsymmetrically functionalize the thieno[2,3-f]benzofuran core at the 2,6 positions as well as to introduce the electron-withdrawing or -donating groups (EWG or EDG) at its 4,8 positions. The presence of various functional groups makes late-stage derivatization attainable.
Synthesis of a 4,8-dialkoxy-benzo[1,2-b:4,5-b′]difuran unit and its application in photovoltaic polymer
Huo, Lijun,Huang, Ye,Fan, Benhu,Guo, Xia,Jing, Yan,Zhang, Maojie,Li, Yongfang,Hou, Jianhui
, p. 3318 - 3320 (2012)
A new building block of benzo[1,2-b:4,5-b′]difuran (BDF) was firstly designed and synthesized. The newly designed unit was applied for constructing a new photovoltaic low band gap polymer, PBDFDTBT, which exhibited promising power conversion efficiency of 5.0%. The Royal Society of Chemistry 2012.
A new benzo[1,2-b:4,5-b′]difuran-based copolymer for efficient polymer solar cells
Chen, Xuewen,Liu, Bo,Zou, Yingping,Xiao, Lu,Guo, Xiuping,He, Yuehui,Li, Yongfang
, p. 17724 - 17731 (2012)
A new donor-acceptor type copolymer, namely poly{4,8-bis(2-ethylhexyloxy) benzo[1,2-b:3,4-b′]difuran-alt-6-octylnaphtho[2,3-c]thiophene-4,9-dione} (PBDFNTDO) was synthesized by a Stille coupling reaction and characterized by 1H NMR, GPC, TGA, UV-Vis absorption spectroscopy and cyclic voltammetry. PBDFNTDO is readily soluble in common organic solvents with a number-average molecular weight (Mn) of 10.7 kDa mol-1 and a polydispersity index of 1.71. TGA analysis shows the copolymer exhibits good thermal stability with 5% weight loss at a temperature of 341 °C. PBDFNTDO possesses a broad absorption band at 300-750 nm with an optical bandgap of 1.65 eV. Cyclic voltammetry gives HOMO and LUMO energy levels of -5.33 eV and -3.40 eV, respectively. The hole mobility of PBDFNTDO:PC71BM (1:1.5, w/w) reaches up to 5.0 × 10-3 cm2 V-1 s -1 by the space-charge-limited current (SCLC) method. A polymer solar cell with the configuration of ITO/PEDOT:PSS/PBDFNTDO:PC71BM (1:1.5, w/w)/Ca/Al demonstrates a promising power conversion efficiency of 4.71% under the illumination of AM 1.5 G, 100 mW cm-2.
Benzamide compound and application thereof as herbicide
-
Paragraph 0059; 0063-0065, (2021/06/12)
The invention discloses a benzamide compound and an application thereof as a herbicide. The compound is shown in a general formula (I) as shown in the specification, and each substituent group in the general formula I is defined in the specification. The
Synthesis of N-trifluoromethyl amides from carboxylic acids
Flavell, Robert R.,Liu, Jianbo,Parker, Matthew F. L.,Toste, F. Dean,Wang, Sinan,Wilson, David M.
supporting information, p. 2245 - 2255 (2021/08/12)
Found in biomolecules, pharmaceuticals, and agrochemicals, amide-containing molecules are ubiquitous in nature, and their derivatization represents a significant methodological goal in fluorine chemistry. Trifluoromethyl amides have emerged as important functional groups frequently found in pharmaceutical compounds. To date, there is no strategy for synthesizing N-trifluoromethyl amides from abundant organic carboxylic acid derivatives, which are ideal starting materials in amide synthesis. Here, we report the synthesis of N-trifluoromethyl amides from carboxylic acid halides and esters under mild conditions via isothiocyanates in the presence of silver fluoride at room temperature. Through this strategy, isothiocyanates are desulfurized with AgF, and then the formed derivative is acylated to afford N-trifluoromethyl amides, including previously inaccessible structures. This method shows broad scope, provides a platform for rapidly generating N-trifluoromethyl amides by virtue of the diversity and availability of both reaction partners, and should find application in the modification of advanced intermediates.
Design and synthesis of heteroaromatic-based benzenesulfonamide derivatives as potent inhibitors of H5N1 influenza A virus
Yu, Yongshi,Tazeem,Xu, Zhichao,Du, Liaoqi,Jin, Mengyu,Dong, Chune,Zhou, Hai-Bing,Wu, Shuwen
, p. 89 - 100 (2019/01/30)
Influenza A virus is an enveloped negative single-stranded RNA virus that causes febrile respiratory infection and represents a clinically challenging threat to human health and even lives worldwide. Even more alarming is the emergence of highly pathogenic avian influenza (HPAI) strains such as H5N1, which possess much higher mortality rate (60%) than seasonal influenza strains in human infection. In this study, a novel series of heteroaromatic-based benzenesulfonamide derivatives were identified as M2 proton channel inhibitors. A systematic investigation of the structure-activity relationships and a molecular docking study demonstrated that the sulfonamide moiety and 2,5-dimethyl-substituted thiophene as the core structure played significant roles in the anti-influenza activity. Among the derivatives, compound 11k exhibited excellent antiviral activity against H5N1 virus with an EC50 value of 0.47 μM and selectivity index of 119.9, which are comparable to those of the reference drug amantadine.
Noncanonical cation-π cyclizations of alkylidene β-ketoesters: Synthesis of spiro-fused and bridged bicyclic ring systems
Parsons, Dylan E.,Frontier, Alison J.
supporting information, p. 2008 - 2012 (2019/03/26)
Three cation-π cyclization cascades initiated at alkylidene β-ketoesters bearing pendent alkenes are described. Depending upon the alkene substitution pattern and the reaction conditions employed, it is possible to achieve selective synthesis of the three different types of products, including 1-halo-3-carbomethoxycyclohexanes, spiro-fused tricyclic systems, and [4.3.1] bridged bicyclic ring systems. All three reactions begin with 6-endo addition of an olefin to the alkylidene β-ketoester electrophile, followed by one of three different cation capture events.
