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Electrochemically enabled functionalization of indoles or anilines to synthesis of hexafluoroisopropoxy indole and anilinederivatives

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00157K, Communication
Zu-yu Mo, Xin-Yu Wang, Yu-zhen Zhang, Li Yang, Hai-Tao Tang, Ying-Ming Pan
An environmentally benign electrochemically enabled site-selective functionalization of indole or aniline derivatives with hexafluoroisopropanol in the presence of tetrabutyl ammonium hexafluorophosphate as redox catalyst and electrolyte was demonstrated in this...
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Synthesis of Glycosyl Sulfoximines by a Highly Chemo- and Stereoselective NH- and O-Transfer to Thioglycosides

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00647E, Paper
Arianna Tota, Claudia Carlucci, Luisa Pisano, Giuliano Cutolo, Guy James Clarkson, Giuseppe Romanazzi, Leonardo Degennaro, James A Bull, Patrick Rollin, Renzo Luisi
A synthesis of unprecedented and stable glycosyl sulfoximines is reported. The developed strategies represent the first examples of highly stereoselective sulfoximine formation directly from thioglycosides. X-ray analysis confirmed the structure...
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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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Copper(I)/Ganphos catalysis: enantioselective synthesis of diverse spirooxindoles using iminoesters and alkyl substituted methyleneindolinones

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00546K, Paper
Hao Cui, Ke Li, Yue Wang, Manman Song, Congcong Wang, Donghui Wei, Er-Qing Li, Zheng Duan, François Mathey
A copper/Ganphos-catalyzed asymmetric 1,3-dipolar cycloaddition of glycine iminoesters with alkyl substituted 3-methylene-2-oxindoles is described, producing the spiro[pyrrolidin-3,3'-oxindole]s in good yields with high ee.
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Origin of the ligand effect in the cobalt catalyzed regioselective hydroboration of 1,3-diene

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00628A, Paper
Yuhua Liu, ZhongJie Jiang, Jipei Chen
The detailed mechanism and the origin of the ligand-controlled regioselectivity in the cobalt catalyzed hydroboration of 2-substituted 1,3-diene have been investigated.
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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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Three-component synthesis of 1,4-benzothiazines via iodide-catalyzed aerobic C–H sulfuration with elemental sulfur

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Org. Biomol. Chem., 2020, 18,3234-3238
DOI: 10.1039/D0OB00074D, Communication
Jingjing Jiang, Xiaolong Tuo, Zhuquan Fu, Huawen Huang, Guo-Jun Deng
Five to Six: Beyond the well-established thiazole formation from elemental sulfur, this method provides the first access to the corresponding six-membered N,S-heterocyclic products via direct functionalization of multiple C–H bonds.
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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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Direct recognition and sensitive detection of circular RNA with ligation-based PCR

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Org. Biomol. Chem., 2020, 18,3269-3273
DOI: 10.1039/D0OB00625D, Communication
Pengbo Zhang, Na Guo, Kejian Gao, Fengxia Su, Fangfang Wang, Zhengping Li
A sensitive and specific method for circRNA detection is developed through the direct ligation of two ingeniously designed DNA probes.
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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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Synthesis of methylene cyclopropane-fused chromenes and dihydroquinolines by sequential [4 + 2]- and [1 + 2]-annulation

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Org. Biomol. Chem., 2020, 18,3303-3311
DOI: 10.1039/D0OB00389A, Paper
Tianyu Lu, Xuange Zhang, Zhiwei Miao
A base promoted sequential [4 + 2]- and [1 + 2]-annulation of 2-hydroxychalcones or 2-tosylaminochalcones with prop-2-ynylsulfonium salts was developed.
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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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Modular continuous flow synthesis of orthogonally protected 6-deoxy glucose glycals

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Org. Biomol. Chem., 2020, 18,3254-3257
DOI: 10.1039/D0OB00522C, Communication
Subbarao Yalamanchili, Tu-Anh V. Nguyen, Nicola L. B. Pohl, Clay S. Bennett
The use of a continuous flow platform for the rapid and highly efficient construction of differentially protected glycals from commercial sources is described.
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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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Base-promoted 1,6-conjugate addition of alkylazaarenes to para-quinone methides

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Org. Biomol. Chem., 2020, 18,3354-3359
DOI: 10.1039/D0OB00419G, Paper
Amritha Rayaroth, Rajat Kumar Singh, Kalyanakrishnan A. V., Krishna Hari, Alagiri Kaliyamoorthy
1,1,2-Triarylethanes embedded with an azaarene unit were prepared in a single step at ambient temperature via the sodium hexamethyldisilazide mediated 1,6-conjugate addition of unactivated alkylazaarenes on para-quinone methides (p-QMs).
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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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Synthesis of phenanthridines by I2-mediated sp3 C–H amination

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Org. Biomol. Chem., 2020, 18,3312-3323
DOI: 10.1039/D0OB00433B, Paper
Benyao Fang, Jiao Hou, Jinyue Tian, Wenquan Yu, Junbiao Chang
An I2-mediated transition-metal-free sp3 C–H amination reaction is established for phenanthridine synthesis in an efficient and scalable manner.
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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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Synthesis of α-CF3-substituted E-dehydroornithine derivatives via copper(I)-catalyzed hydroamination of allenes

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Org. Biomol. Chem., 2020, 18,3274-3280
DOI: 10.1039/D0OB00580K, Paper
Anna N. Philippova, Daria V. Vorobyeva, Florian Monnier, Sergey N. Osipov
Novel α-CF3-substituted E-dehydroornithine derivatives have been synthesized via the Cu(I)-catalyzed hydroamination of α-CF3-α-allenyl-α-aminocarboxylates/phosphonates with different amines.
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KI/TBHP-promoted [3 + 2] cycloaddition of pyrrolo[1,2-a]quinoxalines and N-arylsulfonylhydrazones

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Org. Biomol. Chem., 2020, 18,3360-3366
DOI: 10.1039/D0OB00494D, Paper
Zhen Yang, Jing He, Yueting Wei, Weiwei Li, Ping Liu
A series of diverse fused [1,2,4]triazolo[3,4-c]quinoxalines was obtained by an efficient KI/TBHP-promoted [3 + 2] cycloaddition of pyrrolo[1,2-a]quinoxalines and N-arylsulfonylhydrazones.
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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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Synthesis of gem-difluoroalkenes via nickel-catalyzed allylic defluorinative reductive cross-coupling of trifluoromethyl alkenes with epoxides

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Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00535E, Communication
Xiao-Yu Lu, Run-Chuang Jiang, Jia-Mei Li, Chuang-Chuang Liu, Qing-Qing Wang, Hai-Pin Zhou
A nickel-catalyzed defluorinative reductive cross-coupling of trifluoromethyl alkenes with epoxides has been developed.
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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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Hierarchical Self-Assembly of Azobenzene Dyad with Inverted Amide Connection into Toroidal and Tubular Nanostructures

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Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00833H, Communication
Shiki Yagai, Takuho Saito
Inversion of the connectivity of amide groups in foldable azobenzene dyads with chiral side chains, which can self-assemble into toroids and nanotubes, significantly increases the thermal stability of these aggregates....
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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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DMRC delays inauguration of Yamuna Bank-Noida line

By archive.indianexpress.com
Published On :: Mon, 10 Aug 2009 12:46:35 GMT

Delhi Metro has delayed the inauguration of the Yamuna Bank-Noida line by a month.


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'Treat the refugee issue as a matter of rights'

By timesofindia.indiatimes.com
Published On :: Tue, 24 Jun 2014 06:37:50 IST

The refugee question in the Indian subcontinent dates back to 1947 when India was partitioned. A horrifying feature of the birth of free India – and Pakistan – was the large mass of refugees who were forced to relocate in the most adverse conditions and amidst brutal violence.


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​'Advertising's art of persuasion — political ads will grow': Prasoon Joshi

By timesofindia.indiatimes.com
Published On :: Wed, 25 Jun 2014 00:04:34 IST

Author and advertising authority headed the Titanium Lions jury at 2014's Cannes International Advertising Festival.


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Officials to pay for illegal building: Venkaiah Naidu

By timesofindia.indiatimes.com
Published On :: Mon, 30 Jun 2014 06:15:53 IST

The Centre will push for key reforms including the provision of incentivising civic agencies for good work & making officials concerned accountable for illegal construction or unauthorized development under their jurisdiction.


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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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Indian American Christians condemn assassination of Bhatti

By timesofindia.indiatimes.com
Published On :: Mon, 07 Mar 2011 08:48:31 IST

Strongly condemning the assassination of Shahbaz Bhatti, the Federation of Indian Christians Organisations of North America appealed to Islamabad to bring the perpetrators of the "dastardly" crime to justice.


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Hindu guru convicted of molesting girls in US

By timesofindia.indiatimes.com
Published On :: Mon, 07 Mar 2011 10:09:18 IST

An octogenarian Hindu religious leader, head of a Hindu ashram, one of the largest temples in the US, has been convicted of molesting two young girls.


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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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Yogi launches app to collect data of migrants

By timesofindia.indiatimes.com
Published On :: Sat, 09 May 2020 08:01:29 IST


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E-tokens fail to take off; liquor shops see rush

By timesofindia.indiatimes.com
Published On :: Fri, 08 May 2020 22:36:14 IST

Booze lovers continued to throng liquor shops in the city, even as the e-token system introduced by the Delhi government could not fully take off due to heavy traffic on the designated website.


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Fake sites offer liquor at doorstep in Delhi

By timesofindia.indiatimes.com
Published On :: Sat, 09 May 2020 05:35:30 IST

The excise department has filed a complaint with Crime Branch of Delhi Police against fake websites claiming to deliver liquor at people's doorsteps. The websites became active a day after Delhi government announced an e-token delivery system to avoid chaos at liquor shops.


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