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Ni(II)-Catalyzed vinylic C–H functionalization of 2-acetamido-3-arylacrylates to access isotetronic acids

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00557F, Paper
Biswajit Roy, Eshani Das, Avijit Roy, Dipakranjan Mal
A ligand-free Ni(II)-catalyzed cascade annulation reaction for the synthesis of 4-aryl-substituted isotetronic acids from 2-acetamido-3-arylacrylates via vinylic C–H functionalization is reported.
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Asymmetric trehalose analogues to probe disaccharide processing pathways in mycobacteria

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00253D, Paper
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Hadyn L. Parker, Ruben M. F. Tomás, Christopher M. Furze, Collette S. Guy, Elizabeth Fullam
Chemoenzymatic synthesis of azido-functionalised asymmetric trehalose analogues that are resistant to enzymatic degradation to probe carbohydrate processing pathways in mycobacteria.
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Acylation of oxindoles using methyl/phenyl esters via mixed Claisen condensation – An access to 3-alkylideneoxindoles

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00789G, Communication
Ramdas Sreedharan, Purushothaman Rajeshwaran, Pradeep Kumar Reddy Panyam, Saurabh Yadav, C. M. Nagaraja, THIRUMANAVELAN GANDHI
Predominantly, aggressive acid chlorides and stoichiometric coupling reagents are employed in the acylating process for synthesizing carbonyl tethered heterocycles. Herein, we report simple acyl sources, viz. methyl and phenyl esters...
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The key entity of a DCAR agonist, phosphatidylinositol mannoside Ac1PIM1: its synthesis and immunomodulatory function

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/C9OB02724F, Communication
Yohei Arai, Shota Torigoe, Takanori Matsumaru, Sho Yamasaki, Yukari Fujimoto
We achieved the first synthesis of phosphatidylinositol mannoside Ac1PIM1, and a very potent agonist of an innate immune receptor DCAR is demonstrated.
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Heterologous expression of the trichostatin gene cluster and functional characterization of N-methyltransferase TsnB8

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00617C, Communication
Wei Liu, Vinay Gopal Jannu, Zhiwen Liu, Qingbo Zhang, Xiaodong Jiang, Liang Ma, Wenjun Zhang, Changsheng Zhang, Yiguang Zhu
N-Methyltransferase TsnB8 was demonstrated to catalyze successive methyltransfer reactions in the biosynthesis of trichostatin.
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Donor–acceptor fluorophores as efficient energy transfer photocatalysts for [2 + 2] photodimerization

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/C9OB02735A, Paper
Qing-An Wu, Feng Chen, Chen-Chao Ren, Xue-Fen Liu, Hao Chen, Liang-Xuan Xu, Xiao-Cong Yu, Shu-Ping Luo
Donor–acceptor fluorophores can act as efficient energy transfer photocatalysts to activate enone substrates, realizing photodimerization and isomerization reaction of enone substrates without precious metal photocatalysts.
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Catalyst- and Solvent-Free Efficient Access to N-Alkylated Amines via Reductive Amination using HBPin

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00740D, Communication
ARNAB RIT, Vipin Kumar Pandey, Somnath Bauri
A sustainable approach which works under catalyst- and solvent-free conditions for the synthesis of structurally diverse secondary amines has been uncovered. This one-pot protocol works efficiently at room temperature and...
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A laccase-catalysed tyrosine click reaction

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00650E, Communication
Shinichi Sato, Keita Nakane, Hiroyuki Nakamura
The tyrosine click reaction of peptides/proteins with the tyrosine modification reagent, N-methyl luminol, was catalysed by a laccase in the presence of molecular oxygen (O2) at 37 °C.
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A silver-catalyzed radical ring-opening reaction of cyclopropanols with sulfonyl oxime ethers

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00055H, Paper
Xiaobao Zeng, Xin Wang, Yanan Zhang, Li Zhu, Yu Zhao
A simple and efficient method for the radical ring-opening reaction of cyclopropanols with sulfonyl oxime ethers catalyzed by AgNO3 is developed, affording γ-keto oxime ethers in moderate to good yields.
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Discrimination of cellular developmental states focusing on glycan transformation and membrane dynamics by using BODIPY-tagged lactosyl ceramides

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00547A, Paper
Kenta Arai, Atsuko Ohtake, Shusaku Daikoku, Katsuhiko Suzuki, Yukishige Ito, Kazuya Kabayama, Koichi Fukase, Yoshimi Kanie, Osamu Kanie
Different cellular states were discriminated by analysing either the glycan transformation of exogenously introduced fluorescently tagged probe molecules or fluorescence recovery after photobleaching before conversion.
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Rhodium-Catalyzed ortho-Acrylation of Aryl Ketone O-Methyl Oximes with Cyclopropenones

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00064G, Communication
Yafeng Liu, Yuan Tian, Kexin Su, Xin Guo, Baohua Chen
An efficient Rh-catalyzed ortho-acrylation reaction for the synthesis of chalcones from O-methyl ketoximes and cyclopropenones via C–H bond activation has been described. This cross-coupling reaction exhibits high functional group tolerance...
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Recent Progress on Transition Metal-catalysed Regioselective C–H Transformations Based on Noncovalent Interactions

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00703J, Review Article
Yoichiro Kuninobu, Takeru Torigoe
Transition metal-catalysed C–H transformations are powerful tools to obtain functionalised organic molecules from simple starting materials. To control regioselectivity is one of the most important issues in C–H transformations. Since...
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Synthesis of unsymmetrical benzils via palladium-catalysed α-arylation–oxidation of 2-hydroxyacetophenones with aryl bromides

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00575D, Paper
Open Access
Takanori Matsuda, Souta Oyama
Unsymmetrical benzils are synthesised by a one-pot tandem palladium-catalysed α-arylation and oxidation of 2-hydroxyacetophenones with aryl bromides.
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Enantioselective Synthesis of Indanone Spiro-Isochromanone Derivatives via Dinuclear Zinc-Catalyzed Michael/Transesterification Tandem Reaction

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00541J, Paper
Xiao-Chao Yang, Meng Xu, Jin-Bao Wang, Meng-Meng Liu, Francois Mathey, Yuan-Zhao Hua, Mincan Wang
An enantioselective Michael/transesterification tandem reaction of α-hydroxy indanones with ortho-ester chalcones was realized by dinuclear zinc catalysts. A series of enantiomerically pure spiro[indanone-2,3’-isochromane-1-one] derivatives were obtained in good yields with...
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Synthesis and photophysical properties of selenopheno[2,3-b]quinoxaline and selenopheno[2,3-b]pyrazine heteroacenes

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00718H, Paper
Amol Sonawane, Atsushi Shimozuma, Taro Udagawa, Masayuki Ninomiya, Mamoru Koketsu
In this paper, we report the novel synthesis of three different heterocycles namely 2-arylselenopheno[2,3-b]quinoxaline, 3-(aryl/alkylselanyl)-2-arylselenopheno[2,3-b]quinoxaline and 6-phenyl-7-(arylselanyl)selenopheno[2,3-b]pyrazine derivatives from the corresponding 2,3-dichloroquinoxaline and 2,3-dichloropyrazine derivatives. Further, photophysical properties were investigated...
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Insights into the secondary structures of lactam N-substituted stapled peptides

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00767F, Communication
Aldrin Vasco Vidal, Celia Gonzalez, Stefan Gröger, W Brandt, Jochen Balbach, Carlos Perez, Ludger A. Wessjohann, Daniel G. Rivera
Stapled peptides derived from the Ugi macrocyclization comprise a special class of cyclopeptides with an N-substituted lactam bridge cross-linking two amino acid side chains. Herein we report a comprehensive analysis...
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Protein labeling approach to improve lysosomal targeting and efficacy of antibody–drug conjugates

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Org. Biomol. Chem., 2020, 18,3229-3233
DOI: 10.1039/D0OB00265H, Communication
Ying Han, Yifan Da, Mingjia Yu, Yaping Cheng, Xin Wang, Jiale Xiong, Guoying Guo, Yan Li, Xianxing Jiang, Xiaoqing Cai
An anti-EGFR nanobody was labeled at the C-terminus with a lysosome-sorting NPGY (Asn-Pro-Gly-Tyr) motif via sortase-mediated ligation to enhance the clathrin-mediated endocytosis.
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Synthesis, structures and photophysical properties of hexacoordinated organosilicon compounds with 2-(2-pyridyl)phenyl groups

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Org. Biomol. Chem., 2020, 18,3239-3242
DOI: 10.1039/D0OB00484G, Communication
Shohei Furuta, Toshiaki Mori, Yusuke Yoshigoe, Kohei Sekine, Yoichiro Kuninobu
We synthesised novel air-, water-, heat-, acid-, and base-stable hexacoordinated organosilicon compounds, which contain two C,N-bidentate ligands and form two silafluorene equivalent moieties, with Lewis acid–base interactions.
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Phenylboronic acid-catalyzed tandem construction of S–S and C–S bonds: a new method for the synthesis of benzyl disulfanylsulfone derivatives from S-benzyl thiosulfonates

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Org. Biomol. Chem., 2020, 18,3243-3248
DOI: 10.1039/D0OB00442A, Communication
Raju Jannapu Reddy, Md. Waheed, Gamidi Rama Krishna
A novel and unique phenylboronic acid-catalyzed tandem construction of S–S and C–S bonds via dimerization–sulfonylation has been disclosed for the synthesis of benzyl disulfanylsulfone derivatives.
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The quasi-irreversible inactivation of cytochrome P450 enzymes by paroxetine: a computational approach

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Org. Biomol. Chem., 2020, 18,3334-3345
DOI: 10.1039/D0OB00529K, Paper
Emadeldin M. Kamel, Al Mokhtar Lamsabhi
The potency of paroxetine as a P450 inhibitor is mainly attributed to the availability of two active sites on its structure, its compatibility with P450's active site and the ease of its tight coordination to heme iron.
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Visible light induced 3-position-selective addition of arylpropiolic acids with ethers via C(sp3)–H functionalization

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Org. Biomol. Chem., 2020, 18,3258-3262
DOI: 10.1039/D0OB00480D, Communication
Zi-juan Wan, Xiao-feng Yuan, Jun Luo
Although the 2-position-selective decarboxylative coupling or addition of arylpropiolic acids with cyclic ethers has been intensively investigated, selective functionalization of arylpropiolic acids at the 3-position is still a big challenge.
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A domino annulation approach to 3,4-diacylpyrrolo[1,2-a]pyrazines: decoration of pyrazine units

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Org. Biomol. Chem., 2020, 18,3324-3333
DOI: 10.1039/D0OB00444H, Paper
Anuradha Dagar, Yohan Seo, Wan Namkung, Ikyon Kim
A new one-pot, sequential three-component access to 3,4-diacylpyrrolo[1,2-a]pyrazine was achieved from the reaction of an α-haloketone, azide, and N-substituted pyrrole-2-carboxaldehyde under mild reaction conditions.
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A visible-light-induced “on–off” one-pot synthesis of 3-arylacetylene coumarins with AIE properties

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Org. Biomol. Chem., 2020, 18,3346-3353
DOI: 10.1039/D0OB00479K, Paper
Xinjie Wu, Ming Jia, Mengmeng Huang, Jung Keun Kim, Zheng Zhao, Junkai Liu, Jinhu Xi, Yabo Li, Yangjie Wu
A mild one-pot approach to 3-arylacetylene coumarins with potential AIE activities was developed via photosensitizer-free photocatalysis and thermocatalysis.
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Modular synthesis of oligoacetylacetones via site-selective silylation of acetylacetone derivatives

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Org. Biomol. Chem., 2020, 18,3297-3302
DOI: 10.1039/D0OB00501K, Paper
Parantap Sarkar, Yuya Inaba, Hayato Shirakura, Tomoki Yoneda, Yasuhide Inokuma
Aliphatic oligoketones with tailored carbonyl and substituent sequences were modularly synthesized utilizing site-selective formation of enol silyl ethers. Their unique conformational preferences in solid-state were revealed by X-ray crystallography.
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Copper-catalyzed direct amination of benzylic hydrocarbons and inactive aliphatic alkanes with arylamines

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Org. Biomol. Chem., 2020, 18,3263-3268
DOI: 10.1039/D0OB00491J, Communication
Hua Yao, Bo Xie, Xiaoyang Zhong, Shengzhou Jin, Sen Lin, Zhaohua Yan
A new synthetic method toward direct C–N bond formation through saturated C–H amination of benzylic hydrocarbons and inactive aliphatic alkanes with primary aromatic amines under an inexpensive catalyst/oxidant (Cu/DTBP) system has been developed.
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A base-promoted tandem approach to bicyclic 8-membered ring ketones

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Org. Biomol. Chem., 2020, 18,3249-3253
DOI: 10.1039/D0OB00618A, Communication
Emerson E. F. dos Santos, Gabriela F. P. de Souza, Deborah A. Simoni, Airton G. Salles
A base-promoted tandem route toward unprecedented bicyclic furan/8-membered ring ketones is reported.
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Chemo- and regioselective click reactions through nickel-catalyzed azide–alkyne cycloaddition

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Org. Biomol. Chem., 2020, 18,3374-3381
DOI: 10.1039/D0OB00579G, Paper
Woo Gyum Kim, Seung-yeol Baek, Seo Yeong Jeong, Dongsik Nam, Ji Hwan Jeon, Wonyoung Choe, Mu-Hyun Baik, Sung You Hong
Nickel-catalyzed [3 + 2] cycloaddition reactions of unsymmetrical alkynes and organic azides afford substituted 1,2,3-triazoles with high levels of chemo- and regioselectivity.
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Dipyrazolodioxadiazocines as shelf-stable “ready-to-use” precursors for an in situ generation of enolate-iminium 1,4-dipoles: a straightforward atom-economical approach to pyrazolo[5,1-d][1,3,5]dioxazines

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Org. Biomol. Chem., 2020, 18,3382-3391
DOI: 10.1039/D0OB00451K, Paper
Vladimir E. Zhulanov, Valeria A. Vigovskaya, Maksim V. Dmitriev, Pavel S. Silaichev, Andrey N. Maslivets, Michael Rubin
Generation of cyclic enolate-iminium 1,4-dipoles via thermolysis of dipyrazolodioxadiazocines in the presence of ketones allowed for efficient preparation of pyrazolo[5,1-d][1,3,5]dioxazines.
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Correction: Synthetic-biology-based discovery of a fungal macrolide from Macrophomina phaseolina

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Org. Biomol. Chem., 2020, 18,3392-3392
DOI: 10.1039/D0OB90051F, Correction
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Yohei Morishita, Terutaka Sonohara, Tohru Taniguchi, Kiyohiro Adachi, Makoto Fujita, Teigo Asai
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Controlling the liberation rate of the in situ release of a chemical fuel for the operationally autonomous motions of molecular machines

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00669F, Paper
Chiara Biagini, Giorgio Capocasa, Daniele Del Giudice, Valerio Cataldi, Luigi Mandolini, Stefano Di Stefano
Aminolysis of the anhydride of 2-cyano-2-phenylpropanoic acid can be employed to conveniently regulate the liberation rate of the related acid which, in turn, can be used as a fuel for acid–base operated molecular machines.
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Gold(III)-catalyzed azide-yne cyclization/O–H insertion cascade reaction for the expeditious construction of 3-alkoxy-4-quinolinone frameworks

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00745E, Paper
Jingjing Huang, Han Su, Ming Bao, Lihua Qiu, Yuanqing Zhang, Xinfang Xu
A gold-catalyzed cascade reaction has been developed, and it provides an expeditious access to 3-alkoxy-4-quinolines and applications in alkaloid synthesis.
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A Selectfluor-promoted oxidative reaction of disulfides and amines: access to sulfinamides

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00720J, Paper
Haibo Mei, Jiang Liu, Romana Pajkert, Gerd-Volker Röschenthaler, Jianlin Han
An unprecedented metal-free oxidative reaction of disulfides and amines with Selectfluor as a mild oxidant under aerobic conditions was developed.
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Late-stage synthesis and application of photoreactive probes derived from direct benzoylation of heteroaromatic C–H bonds

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00336K, Communication
Kevin D. Hesp, Jun Xiao, Graham M. West
A synthetically-driven, late-stage C–H benzoylation strategy for the expedited preparation and evaluation of heterocyclic alternatives to more classical benzophenone photoreactive probes is reported.
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Dienaminodioate based multicomponent reactions with post-benzylic oxidative transformations mediated by DDQ

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00721H, Paper
Jaice Ravindran, Velickakathu Yadhukrishnan, Reghuvaran Asha , Ravi Shankar Lankalapalli
Multicomponent reactions (MCRs) using dienaminodioate with post-benzylic oxidative transformation by DDQ that afforded a diverse array of products is described. An unprecedented rearrangement of 1,2-dihydropyridines (1,2-DHPs), 3CR products, to 2-pyridones...
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Arylation of Indoles Using Cyclohexanones Dually-Catalyzed by Niobic Acid and Palladium-on-Carbons

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00702A, Paper
Kazuho Ban, Yuta Yamamoto, Hironao Sajiki, Yoshinari Sawama
3-Arylindoles were easily constructed from indoles and cyclohexanone derivatives using a combination of catalytic niobic acid-on-carbon (Nb2O5/C) and palladium-on-carbon (Pd/C) under heating conditions without any oxidants. The Lewis acidic Nb2O5/C...
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Correction: Nickel-catalyzed cyanation of phenol derivatives activated by 2,4,6-trichloro-1,3,5-triazine

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB90052D, Correction
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Liang Wang, Yaoyao Wang, Jun Shen, Qun Chen, Ming-Yang He
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Efficient synthesis of a galectin inhibitor clinical candidate (TD139) using a Payne rearrangement/azidation reaction cascade

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00910E, Paper
Jacob St-Gelais, Vincent Denavit, Denis Giguère
Selective galectin inhibitors are valuable research tools and could also be used as drug candidates. In that context, TD139, a thiodigalactoside galectin-3 inhibitor, is currently being evaluated clinically for the...
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70 per cent of teachers in Delhi schools are obese: survey

By archive.indianexpress.com
Published On :: Tue, 04 Aug 2009 12:27:25 GMT

Nearly 70 per cent of schoolteachers in the national capital are overweight and obese, a recent survey has claimed.


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Aspiring actor-cum-model arrested for killing IT professional

By archive.indianexpress.com
Published On :: Thu, 06 Aug 2009 14:26:17 GMT

A 20-year-old aspiring actor- cum-model was arrested in the national capital for allegedly murdering a young woman IT professional a week ago after she refused to heed to his demand for money.


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We’ll look back at 2014 as a new journey for India-Israel ties: Alon Ushpiz

By timesofindia.indiatimes.com
Published On :: Fri, 13 Jun 2014 00:08:59 IST

India and Israel have signed a far-reaching agreement on homeland security where the two countries will collaborate on policing, forensics, counter-terrorism, etc. Israel's ambassador Alon Ushpiz spoke with Indrani Bagchi about shared concerns, PM Modi — and justice in the 2012 attack on an Israeli diplomat:


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Progress measures must include nature — think beyond GDP: Rachel Kyte

By timesofindia.indiatimes.com
Published On :: Fri, 20 Jun 2014 00:06:10 IST

As India debates environmental health versus economic growth, Rachel Kyte, vice-president and special envoy for climate change at the World Bank Group, feels it is vital to think beyond basic GDP.


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Women suffer sanitation absence most — also impacts economy: Bindeshwar Pathak

By timesofindia.indiatimes.com
Published On :: Fri, 27 Jun 2014 00:06:33 IST

One month after the horrific Badaun gang rape exposed how gravely at risk women and minors lacking domestic toilets are.


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A strong and vibrant India is important for peace and stability in Asia: K Shanmugam, Singapore's foreign minister

By timesofindia.indiatimes.com
Published On :: Fri, 04 Jul 2014 16:34:46 IST

Singapore is one of India's closest partners in Asia. In his first visit to meet PM Narendra Modi after the formation of the NDA government, K Shanmugam, Singapore's foreign minister, tells Indrani Bagchi they would build some of India's new smart cities and involve themselves in skill development programmes in India.


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Swiss accounts are a diversion. Bulk of black money is right here in India

By timesofindia.indiatimes.com
Published On :: Sun, 06 Jul 2014 06:49:59 IST

The scent of 'black money' is in the air again. At the Supreme Court's order, Modi sarkar has set up a Special Investigation Team to look into cases of illegal outflow of money to foreign havens.


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Hate crime: Two Sikhs attacked in US, one dead

By timesofindia.indiatimes.com
Published On :: Mon, 07 Mar 2011 09:00:29 IST

Two elderly Sikhs were shot at by unidentified assailants in Sacramento in US, leaving one dead and the other in critical condition, triggering panic in the neighbourhood having a sizeable Sikh population.


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NRI dentist in UK faces charges of seducing patient

By timesofindia.indiatimes.com
Published On :: Tue, 15 Mar 2011 18:09:24 IST

An NRI dentist, once the face of Oral B toothpaste and appears on a British TV show, has been accused of seducing a patient on the couch of his dental clinic and marital home, a disciplinary hearing was told.


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Indian-origin model accuses Aus modelling agency of racism

By timesofindia.indiatimes.com
Published On :: Wed, 16 Mar 2011 13:41:31 IST

According to a report in the local daily, Kema Rajandran was told by a Parth-based modelling agency that her work chances were "limited" in the country because she was not Caucasian.


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Indian teachers in demand in Singapore

By timesofindia.indiatimes.com
Published On :: Thu, 07 Apr 2011 12:55:27 IST

Indian teachers are most sought after in Singapore schools with increasing number of teachers being recruited to teach not only Indian languages but also other subjects.


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Lucknow zoo animals are more active in lockdown

By timesofindia.indiatimes.com
Published On :: Fri, 08 May 2020 04:45:00 IST


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UP: 1 dies, 6 hurt in three accidents on e-way

By timesofindia.indiatimes.com
Published On :: Fri, 08 May 2020 21:18:30 IST

Three back-to-back road accidents on Agra-Lucknow Expressway on Friday left one dead and many injured.


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