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BODIPY(aryl)iodonium salts in the efficient synthesis of diversely functionalized BODIPYs and selective detection of serum albumin

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00336E, Paper
Open Access
Bintu Kumar, Anindita Bhatta, Prakriti Saraf, Taur Prakash Pandurang, Krishnan Rangan, Madhushree Sarkar, Sivaprasad Mitra, Dalip Kumar
Using readily available BODIPY and iodoarenes various BODIPY(aryl)iodonium salts were prepared and successfully utilized for the direct syntheses of functionalized BODIPYs, bis-BODIPYs and for the selective detection of serum protein.
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Coumarin–azasugar–benzyl conjugates as non-neurotoxic dual inhibitors of butyrylcholinesterase and cancer cell growth

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00312H, Paper
I. Caroline Vaaland Holmgard, Aday González-Bakker, Eleonora Poeta, Adrián Puerta, Miguel X. Fernandes, Barbara Monti, José G. Fernández-Bolaños, José M. Padrón, Óscar López, Emil Lindbäck
Coumarin–azasugar–benzyl conjugates were obtained through the CuAAC reaction, displaying dual anti-Alzheimer and anti-cancer activity in vitro and no neurotoxicity.
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Diastereoselective synthesis of functionalized spiroindolines via intramolecular ipso-iodocyclization/nucleophile addition cascade reactions of indole-tethered ynones

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00112E, Paper
Debojyoti Bag, Sanghapal D. Sawant
Herein, we describe a highly diastereoselective approach for synthesizing polyfunctionalized spiroindolines from indolyl-ynones involving an ipso-iodocyclization/nucleophile addition cascade.
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Kinetic resolution of 1,1'-binaphthyl-2,2'-diamine derivatives by chiral calcium phosphate-catalyzed acylation

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00355A, Paper
Tatsuhiro Uchikura, Yuki Kanno, Yukino Fukuda, Mikoto Sato, Takahiko Akiyama
Chiral calcium phosphate-catalyzed kinetic resolution of BINAM derivatives.
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Copper catalyzed dehydrogenative cyclization, alkenylation towards dihydroquinolinones

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00134F, Paper
Pari Keerthana, Fazlur-Rahman Nawaz Khan
An efficient copper-catalysized one-pot sequential synthesis of alkenylated quinolinyldihydroquinolinones is reported utilizing ketones, 1,3-cyclohexanediones, and benzyl alcohols via dehydrogenative cyclisation, followed by alkenylation. This highly straightforward method provides a mild...
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An efficient synthesis of mono-, di-, and tri-substituted 1,3-thiazoles employing functionalized thioamides as thiocarbonyl precursors

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00229F, Paper
Kalleshappa Sheela, Chikkappaiahnayaka Santhosh, Krishna Ravi Singh, Kalleshappa Sharath, Maralinganadoddi P. Sadashiva
Herein, we report an efficient strategy to synthesize functionalized 1,3-thiazoles using alkyl 2-amino-2-thioxoacetates.
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A rhodium-catalyzed cascade C–H activation/annulation strategy for the expeditious assembly of pyrrolidinedione-fused 1,2-benzothiazines

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00193A, Paper
Yinsong Wu, Guanghao Shi, Yanan Liu, Yangzilin Kong, Mengdi Wu, Demao Wang, Xiaobing Wu, Yongjia Shang, Xinwei He
We have developed a cascade annulation strategy triggered by rhodium(III)-catalyzed C–H activation for the expeditious assembly of pyrrolidinedione-fused 1,2-benzothiazines from free NH-sulfoximines with maleimides under mild conditions.
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Generation of sulfones utilizing β-sulfinyl esters as masked aryl sulfinates under redox-neutral conditions

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00238E, Communication
Yixin Zhang, Zhu Yang, Hongjun Yang, Xuefeng Li, Lu Yang
A method for generation of SVI sulfones from β-sulfinyl esters (SIV) under transition-metal-free non-oxidative mild conditions is presented.
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Photoinduced decatungstate-catalyzed C(sp3)–H thioetherification by sulfinate salts

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00394B, Paper
Pengcheng Li, Jia-Lin Tu, Ao-Men Hu, Lin Guo, Chao Yang, Wujiong Xia
A visible light photoinduced decatungstate-catalyzed C(sp3)–H thioetherification of hydrocarbons by sodium sulfite is herein reported.
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A copper-catalyzed asymmetric Friedel–Crafts hydroxyalkylation of pyrazole-4,5-diones with 5-aminoisoxazoles

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00322E, Communication
Siyu Gao, Xiang Sun, Sijie Peng, Zhenggen Zha, Qi Sun, Zhiyong Wang
An asymmetric Friede-Crafts hydroxyalkylation reaction was developed under the catalysis of chiral copper complexes. A variety of pyrazolone derivatives were obtained with excellent yields and enantioselectivities.
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Copper-catalyzed ortho-thiocyanation of aromatic amines

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00137K, Communication
Monak Patel, Nitish Kumar, Hussain Bhukya, Bharatkumar Z. Dholakiya, Togati Naveen
Here, we described an efficient ortho- C(sp2)-H thiocyanation of anilines for the synthesis of aryl thiocyanates. This protocol tolerates a variety of aromatic amines to provide the desired products in good to excellent yields.
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Chemoenzymatic total synthesis of rotigotine via IRED-catalyzed reductive amination

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00072B, Communication
Dongyu Tang, Yaqing Ma, Jinping Bao, Shushan Gao, Shuli Man, Chengsen Cui
An engineered imine reductase (IRED) was developed specifically for 2-tetralone substrate, and utilized in the total synthesis of rotigotine.
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Rh(III)-catalysed C-H annulation of cis-stilbene acids with 2-diazo-1,3-diketones: A facile access to 6,7-dihydrobenzofuran-4(5H)-one and α-pyrone scaffolds

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00151F, Paper
Shankaraiah Nagula, Mary Sravani Galla, Nandini B. Kale, Akshay Kumawat, Darshana Bora
An efficient Rh(III)-catalysed C-H functionalization, tandem annulation of cis-stilbene acids using 2-diazo-1,3-diketones was devised. The protocol has solely afforded 6,7-dihydrobenzofuran-4(5H)-ones using alicyclic diazocarbonyls via decarbonylation and α-pyrones with aliphatic diazo...
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DMSO promoted catalyst-free oxidative C–N/C–O couplings towards synthesis of imidazoles and oxazoles

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00383G, Paper
Debasish Bera, Rajib Sarkar, Tiyasa Dhar, Pinaki Saha, Prasanta Ghosh, Chhanda Mukhopadhyay
Dimethyl sulfoxide (DMSO)-promoted catalyst-free oxidative C–N coupling and C–O coupling under oxidant-free conditions are outlined.
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Electrochemical nickel-catalyzed cross-coupling of glycosyl thiols with preactivated phenols and ketones

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00442F, Communication
Fuxin Li, Hui Liu, Wanyu Xing, Qingju Zhang, Liming Wang
Here we report an efficient electrochemical nickel-catalyzed cross-coupling reaction for the synthesis of S-glycosides from preactivated phenols and ketones.
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Stereoselective Synthesis of gem-Dihalopiperidines via Halo-Aza-Prins Cyclization Reaction: Access to Piperidin-4-ones and Pyridines

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00338A, Paper
Anil Kumar Saikia, Surjya Kumar Bora, Subhamoy Biswas, Bipin Kumar Behera
An efficient methodology for the synthesis of 4,4-dihalopiperidine derivatives has been developed from N-(3-halobut-3-en-1-yl)-4-methylbenzenesulfonamide and aldehyde catalyzed by In(OTf)3 in excellent yields. The reaction involves an initial formation of six...
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Reduction of sulfoxides catalyzed by the commercially available manganese complex MnBr(CO)5

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00204K, Paper
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Daniel Leal Lourenço, Ana Cristina Fernandes
A new methodology for the reduction of a wide variety of aliphatic and aromatic sulfoxides catalyzed by the air-stable, cheap and commercially available manganese catalyst MnBr(CO)5 with excellent yields is...
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Covalently linked thieno[2,3-b]thiophene-fullerene dimers: synthesis and physical characterization

Org. Biomol. Chem., 2024, 22,2978-2984
DOI: 10.1039/D4OB00027G, Paper
Abdulrahman M. Alazemi, Mohammad H. BinSabt, Hamad M. Al-Matar, Alan L. Balch, Mona A. Shalaby
Linked thieno[2,3-b]thiophene-fullerene Dimers.
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Asymmetric synthesis of the fully functionalized six-membered A-ring of siphonol A

Org. Biomol. Chem., 2024, 22,2958-2962
DOI: 10.1039/D4OB00104D, Communication
Ying Sun, Shaomin Fu, Bo Liu
The asymmetric synthesis of the fully functionalized six-membered A-ring of siphonol A is presented.
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Recent advances in spirocyclization of maleimides via transition-metal catalyzed C–H activation

Org. Biomol. Chem., 2024, 22,2916-2947
DOI: 10.1039/D3OB01904G, Review Article
Swadhin Swaraj Acharya, Sagarika Patra, Rojalini Maharana, Manaswini Dash, Liza Mama Barad, Bibhuti Bhusan Parida
In recent years, the maleimide scaffold has received a great deal of attention in C–H activation.
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2-Azabicyclo[3.2.1]octane scaffold: synthesis and applications

Org. Biomol. Chem., 2024, 22,2902-2915
DOI: 10.1039/D4OB00199K, Review Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Mariana Crespo Monteiro, João Rafael Vale, Filipa Siopa
This review focuses on the preparation and applications in total synthesis of 2-azabicyclo[3.2.1]octane structures, a class of natural and synthetic compounds with a range of biological activities.
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Hydrosilylation of nitriles and tertiary amides using a zinc precursor

Org. Biomol. Chem., 2024, 22,3053-3058
DOI: 10.1039/D4OB00161C, Paper
Ravi Kumar, Rohan Kumar Meher, Himadri Karmakar, Tarun K. Panda
A competent and selective hydrosilylation of nitriles and tertiary amides catalyzed by zinc bis(hexamethyldisilazide) [Zn(HMDS)2] under solvent-free and mild conditions are reported, as a sustainable and desirable alternative to existing methods.
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Expanding the scope of the successive ring expansion strategy for macrocycle and medium-sized ring synthesis: unreactive and reactive lactams

Org. Biomol. Chem., 2024, 22,2985-2991
DOI: 10.1039/D4OB00285G, Paper
Open Access
Zhongzhen Yang, Marion Arnoux, Damien Hazelard, Owen R. Hughes, Joe Nabarro, Adrian C. Whitwood, Martin A. Fascione, Christopher D. Spicer, Philippe Compain, William P. Unsworth
New Successive Ring Expansion (SuRE) protocols are described for use on unreactive lactams, as well as iminosugar derived lactams.
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Photogenerated chlorine radicals activate C(sp3)–H bonds of alkylbenzenes to access quinazolinones

Org. Biomol. Chem., 2024, 22,2968-2973
DOI: 10.1039/D4OB00129J, Communication
Xin-Yao Pan, Gui-Xia Sun, Fang-Ping Huang, Wen-Jian Qin, Qing-Hu Teng, Kai Wang
An Fe-catalyzed visible-light induced condensation of alkylbenzenes with anthranilamides has been developed.
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Palladium-catalyzed (Z)-selective allylation of phosphine oxides with vinylethylene carbonates to construct phosphorus allyl alcohols

Org. Biomol. Chem., 2024, 22,3068-3072
DOI: 10.1039/D4OB00354C, Paper
Hua Huang, Yi-Qi Wu, Lu-Yao Han, Lu Jiang, Zhuo-Zhuo Zhang, Xiang Zhang, Bo Han, Wei Huang, Jun-Long Li
A general and efficient method for the highly stereoselective synthesis of (Z)-phosphorus allylalcohols has been developed using the Pd-catalyzed cross-coupling of phosphine oxides with vinylethylene carbonates.
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Stereoselective synthesis of (R)- and (S)-1,2-diazetidine-3-carboxylic acid derivatives for peptidomimetics

Org. Biomol. Chem., 2024, 22,2974-2977
DOI: 10.1039/D4OB00278D, Communication
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Matthew Nutter, Henry Stone, Michael Shipman, Stefan Roesner
Stereoselective synthesis of both enantiomers of orthogonally protected 1,2-diazetidine-3-carboxylic acid (aAze) from homochiral glycidol and its application in peptidomimetics.
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Iron-catalyzed selective construction of indole derivatives via oxidative C(sp3)–H functionalization of indolin-2-ones

Org. Biomol. Chem., 2024, 22,3073-3079
DOI: 10.1039/D4OB00133H, Paper
Wei Chen, Lang-Qi Wen, Xiao-Bing Lu, Hui Zhou
We have developed a clean and efficient iron-catalyzed C(sp3)–H functionalization of indolin-2-ones for the chemodivergent synthesis of value-added indole derivatives, including isatins, and symmetrical and non-symmetrical isoindigos.
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Photochromism of phenazine-2,3-diol derivatives through excited state intermolecular proton transfer based on keto–enol tautomerization

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00387J, Paper
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Kazuki Ohira, Kumpei Kozuka, Naoki Kaneda, Masahiro Yamamoto, Keiichi Imato, Yousuke Ooyama
It was found that phenazine-2,3-diol derivatives exhibit photochromism through excited state intermolecular proton transfer (ESInterPT) processes based on keto–enol tautomerization.
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BBr3-mediated dearomative spirocyclization of biaryl ynones: facile access to spiro[5.5]dienones

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00274A, Communication
Gaurav Jaiswal, Subhas Chandra Pan
BBr3 mediated dearomative spirocyclization of biaryl ynones has been reported for the direct synthesis of spiro[5.5]dienones with a tri-substituted double bond.
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3-Halo-5,6-dihydro-4H-1,2-oxazine N-oxides as synthetic equivalents of unsaturated nitrile oxides in the [3 + 2]-cycloaddition with arynes: synthesis of substituted 3-vinyl-1,2-benzisoxazoles

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00391H, Communication
Alexander A. Lukoyanov, Svetlana A. Aksenova, Andrey A. Tabolin, Alexey Yu. Sukhorukov
3-Halo-1,2-oxazine N-oxide derivatives act as surrogates of vinyl nitrile oxides in tandem [3 + 2]-cycloaddition/[3 + 2]-cyclofragmentation with arynes leading to benzisoxazoles.
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Cu(OTf)2/HFIP catalyzed regioselective cycloisomerization of indole-C3-functionalized alkynols to carbazoles

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00421C, Communication
Srinivasarao Yaragorla, Tabassum Khan, Sayonika Chakroborty
We report here a simple and atom economic cycloisomerization reaction of indole-tethered alkynols for constructing diverse carbazoles via 1,2-alkly migration using Cu(OTf)2/HFIP as the excellent promoter system.
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Electro-oxidative three-component cascade coupling of isocyanides with elemental sulfur and amines for the synthesis of 2-aminobenzothiazoles

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00432A, Paper
Peng-Fei Huang, Jia-Le Fu, Ying Peng, Jian-Hong Fan, Long-Jin Zhong, Kewen Tang, Yu Liu
2-Aminobenzothiazoles are commonly encountered in various functional compounds. Herein, we disclose an electro-oxidative three-component reaction for the effective synthesis of 2-aminobenzothiazoles under mild conditions, utilizing non-toxic and abundant elemental sulfur...
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Recent developments in the enzymatic modifications of steroid scaffolds

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00327F, Review Article
Open Access
Huibin Wang, Ikuro Abe
This review highlights the recent advancements in the enzymatic modifications of steroid scaffolds, emphasizing enzymatic hydroxylation, ketoreduction, dehydrogenation, enzymatic cascade reactions, and other modifications.
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An FeCl3-catalyzed three-component reaction for the synthesis of β-(1,2,3-triazolyl)-ketones using DMF as a one-carbon source

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00207E, Communication
Ruilin Fang, Lei Zheng, Xuyang Chen, Can Wang, Yunfeng Chen
FeCl3-catalyzed oxidative condensation of NH-1,2,3-triazoles and aryl methyl ketones and DMF has been reported.
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A Highly Diastereoselective One-Pot Ugi/Radical Spirocyclization/Aza-Michael Addition Sequence

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00610K, Communication
Chandra Volla, Salman Khan, Abhradeep Chatterjee, Akshay Murali Nair
We hereby report a highly diastereoselective synthesis of chalcogenated azaspirotricycles via a one-pot Ugi/spirocyclization/ aza-Michael addition sequence. The reaction proceeded via a key visible light mediated spirocyclization step under mild,...
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New Generation of Highly Reactive Allylborating Agents For Cu(I)-Catalyzed Allylation of Chiral Sulfinylimines

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00291A, Paper
Michael S. Alexeev, Tatyana V. Strelkova, Michail M. Ilyin, Jr., Yulia V. Nelyubina, Ivan A. Bespalov, Michael Medvedev, Victor N Khrustalev, Nikolai Kuznetsov
The implementation of selective catalytic processes with highly active reagents is an attractive strategy that meets modern principles of sustainable development of chemistry. In the current study, we for the...
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N-Functionalization of beta-aminophosphonates; Cytotoxic effect of the new derivatives

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00243A, Paper
György Keglevich, Petra Regina Varga, Emőke Dinnyési, Zsuzsanna Szalai, Szilvia Bősze, Rita Oláhné Szabó, Laszlo Drahos, Konstantin Karaghiosoff
Beta-Aminophosponates obtained by the Michael addition of primary amines to the double bond of diethyl vinylphosphonate proved to be suitable starting materials (amine components) in the Kabachnik–Fields reaction with formaldehyde...
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Sustainable preparation of 2-acylbenzothiazoles under the cooperation of ionic liquids and microwave irradiation

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00315B, Paper
Shoushun Wang, Mengjie Liu, Yiyuan Yue, Xiude Hu, Yalin Zhang, Guodong Shen, Ruiguo Dong, Lilong Shi, Bing Yu, Xianqiang Huang
A series of 2-acylbenzothiazole derivatives were sustainably synthesized for the first time under the cooperation of ionic liquids and microwave irradiation, metal- and extra-additives-free conditions.
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Tetrabutylammonium decatungstate (TBADT), a compelling and trailblazing catalyst for visible-light-induced organic photocatalysis

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00171K, Review Article
Bor-Cherng Hong, Ranadheer Reddy Indurmuddam
This review summarizes recent developments in visible-light or near-visible-light photocatalysis reactions enabled by the TBADT catalyst.
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Base- and sulfur-promoted oxidative lactonization of chalcone-acetate Michael adducts: access to pyran-2-ones

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00479E, Communication
Cao Nguyen Nguyen, Duc Toan Nguyen, Ha An Tran, Dinh Hung Mac, Thi Thu Tram Nguyen, Pascal Retailleau, Thanh Binh Nguyen
A cost-effective, practical, straightforward and scalable synthesis of α-pyrones via base- and sulfur-promoted annulation of phenylacetates and chalcones is reported.
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Visible light-driven photocatalytic sulfonative oxidation of benzyl secondary amines

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00348A, Paper
Yong-Xiang Lü, Xinqian Wang, Ying-Ming Pan, Keyume Ablajan
A method for the α-oxidation and sulfonation of benzyl secondary amines was developed utilizing Ir(III) or Eosin Y as the photocatalyst in the presence of O2 as a green oxidant....
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A time when hijackings were dime-a-dozen in the US

Unthinkable in today’s hyper-security post-9/11 environment, forced diversions were commonplace in the ’60s




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Why Mount Everest is a no-fly zone

Hurricane-force winds and frequent snowstorms are obstacles




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Mission to Net Zero: Aviation’s focus on making sustainable connections 

Flying the cleanest, greenest, youngest fleet possible can be a way towards the goal 




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Zomato users can now schedule order 2 days in advance

Zomato’s order scheduling is available at more than 35,000 restaurants across 30 cities




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As Bitcoin nears all-time high, WazirX investors are in pain over their locked crypto funds

Bitcoin was inching towards its March 2024 all-time-high price of $73,750.07, but those whose crypto assets are locked with the WazirX exchange after a cyberattack are anxious about missing out




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Microsoft, Meta, Apple, Amazon, and the burden of expectations knock Wall Street sharply lower

Drops for Big Tech companies including Microsoft and Facebook’s parent company Meta Platforms led Wall Street lower




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Amazon's improving retail sales boost third-quarter profit, revenue beats estimates

Like its tech peers, Amazon said it expected higher capital expenditures for the foreseeable future to help develop artificial intelligence software




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Amazon won’t release new Alexa until 2025: Report

Until sometime ago, users were able to access the beta version of Alexa using an Echo but that has been cut off now




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I Didn’t Realize How Much I Rely on GitHub Codespaces Until This week

How much do I rely on GitHub Codespaces for open source development? Super double-plus much. I can illustrate exactly how much with one short anecdote. Gulp 5 was recently released and I created several PRs across repos in the H5BP organization to update Gulp across the board. I missed one issue with the encoding of […]