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Structural flexibility of favipiravir and its structural analogues in solutions: experimental and computational insight

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00404C, Paper
Tatiana P. Gerasimova, Almaz A. Zagidullin, Anastasiia N. Nikolaeva, Robert R. Fayzullin, Aliya M. Saitova, Vasili A. Miluykov, Stefan Grimme, Sergey A. Katsyuba
Keto-enol transformations of 6-R-3-hydroxy-2-pyrazinecarboxamides in solutions are accompanied by deprotonation of enol tautomers and the formation of corresponding anionic species. The key factors determining these processes have been identified.
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Catalyst- and base-free visible light-enabled radical relay trihalomethylation/functional group-migration/carbonylation with CX3SO2Cl

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00292J, Paper
Jinkai Hu, Chenglei Yang, Xiaotao Qin, Hui Liu, Tongtong Ma, Ao-tong Shi, Qing-Long Lv, Xingman Liu, Jinhui Yang, Dianjun Li
A visible light-enabled photocatalyst-free radical trihalomethylation/cyano (or benzo[d]thiazol-2-yl) 1,4-migration/carbonylation reaction of 2-hydroxy-2-hex-5-enenitrile (or (benzo[d]thiazol-2-yl)-pent-4-enol) with CX3SO2Cl (X = F, Cl) is reported.
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Total synthesis of diplofuranone A and diapolic acid A

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00433G, Communication
Dattatraya H. Dethe, Vimlesh Kumar, Nagabhushana C. Beeralingappa
The first and concise syntheses of the anticancer agent diplofuranone A and the fatty acid-derived metabolite diapolic acid A have been demonstrated using easily accessible and commercially available starting materials.
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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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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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Vinylogous and stereoselective domino synthesis of pyrano[2,3-c]pyrroles from alkylidene meldrum's acids

Org. Biomol. Chem., 2024, 22,2948-2952
DOI: 10.1039/D4OB00233D, Communication
Mariia Savchuk, Giang Vo-Thanh, Sylvain Oudeyer, Hélène Beucher, Jean-François Brière
An expeditious diatereoselective synthesis of pyrano[2,3-c]pyrroles thanks to a domino Vinylogous aza-Michael-Aldol-Cyclocondensation (aza-VMAC) reaction to alkylidene Meldrum's acid derivatives.
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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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Not exclusively the activity, but the sweet spot: a dehydrogenase point mutation synergistically boosts activity, substrate tolerance, thermal stability and yield

Org. Biomol. Chem., 2024, 22,3009-3018
DOI: 10.1039/D4OB00211C, Paper
Yu-Ke Cen, Lin Zhang, Yue Jiang, Xiang-Fu Meng, Yuan Li, Chao Xiang, Ya-Ping Xue, Yu-Guo Zheng
A single-point mutation of 7α-HSDH achieved the highest activity and synergistically improved substrate tolerance, thermal stability, cofactor affinity, and conversion rate.
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Selective synthesis of an elusive C-functional bis-cyclam and study of its inhibition of the CXCR4 chemokine receptor

Org. Biomol. Chem., 2024, 22,3059-3067
DOI: 10.1039/D3OB02050A, Paper
Marie M. Le Roy, Sandra Claes, Nathalie Saffon-Merceron, Dominique Schols, Thibault Troadec, Raphaël Tripier
A rare example of C,C'-linked bis-cyclam has been synthesized with controlled manner in mild conditions thanks to the “bis-aminal” tool, and its good CXCR4-recognition properties could be demonstated in vitro.
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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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Unusual immunosuppressive pyridine-containing bisnor- (c23), tetranor- (c21) and pentanor- (c20) sesterterpenoids from Tibetan Leucosceptrum canum

Org. Biomol. Chem., 2024, 22,3019-3024
DOI: 10.1039/D4OB00334A, Paper
Man Li, Ling Feng, Han Zhang, Yan-Chun Liu, Ting-Ting Zhou, Yu Zheng, Kai Guo, Yan Liu, Sheng-Hong Li
Six unusual pyridine-containing bisnor- (C23), tetranor- (C21) and pentanor- (C20) sesterterpenoids were obtained from the medicinal plant Leucosceptrum canum of Tibetan origin. The immunosuppressive activities of these sesterterpenoids were observed.
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A phosphamide nucleotide analog: a substrate for polymerase synthesis of DNA

Org. Biomol. Chem., 2024, 22,2963-2967
DOI: 10.1039/D4OB00089G, Communication
Jiong Meng, Qiaqia Guo, Xiaona Zhai, Song Yang, Shuai Wang, Pengcheng Wang, Debin Ji
A phosphamide nucleotide analog (dNTPγNH2) exhibited higher stability than dNTPs and can be recognized by DNA polymerases in PCR.
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Synthesis of alkynyl sulfides via base-promoted nucleophilic ring-opening of α-bromostyrene sulfonium salt

Org. Biomol. Chem., 2024, 22,2953-2957
DOI: 10.1039/D4OB00203B, Communication
Junqi Zhou, Ziyu Wang, Hanmiao Xu, Mengke Su, Jian Wen
An effective method for synthesizing various alkynyl sulfides has been developed using tetramethylene sulfoxide as a sulfur source through base-promoted nucleophilic ring-opening reactions.
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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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Charge-transfer inclusion complex formation of the tropylium cation with prism[6]arenes

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00423J, Communication
Guojiao Zhang, Channi Cheng, Zhengxiang Li, Dezhi Zhao, Chengyou Han
We report that charge-transfer (CT) inclusion complexes were formed between prism[6]arenes and tropylium cation. Additionally, the CT complex showed Cl/Ag+ responsiveness which can be easily monitored by the naked eye.
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Nickel-catalysed regio- and stereoselective hydrocyanation of alkynoates and its mechanistic insights proposed by DFT calculations

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00380B, Communication
Shigeru Arai, Koichi Nakazawa, Xiao-Fei Yang, Masaya Nakajima, Shinji Harada, Atsushi Nishida
This work discloses the origin of regio- and stereoselectivity of hydrocyanation of alkynoates.
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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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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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Revisiting Biginelli-like Reactions: Solvent Effects, Mechanisms, Biological Applications and Correction of Several Literature Reports

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00272E, Paper
Brenno A. D. Neto, Pedro Beck, Arthur Leitão, Yasmin Santana, Jose R. Correa, Carime Vitória da Silva Rodrigues, Daniel Machado, Guilherme Matos, Luciana Machado Ramos, Claudia Cristina Gatto, Carlos Kleber Z. Andrade, Sarah Caldas
This study critically reevaluates reported Biginelli-like reactions using a Kamlet-Abboud-Taft-based solvent effect model. Surprisingly, structural misassignments were discovered in certain multicomponent reactions, leading to the identification of pseudo three-component derivatives...
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Design, synthesis, biological evaluation and molecular docking studies of quinoline-anthranilic acid hybrids as potent anti-inflammatory drugs

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00040D, Paper
Sidra Siddique, Khalid Hussain, Naureen Shehzadi, Muhammad Arshad, Muhammad Nadeem Arshad, Sadaf Iftikhar, Farhat Saghir, Ayisha Shaukat, Muhammad Sarfraz, Nisar Ahmed
Despite the high global prevalence, rheumatoid arthritis lacks a satisfactory treatment.
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Isothiocyanates: Happy-Go-Lucky Reagents in Organic Synthesis

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00281D, Review Article
Bubul Das, Anjali Dahiya, Bhisma K Patel
: Owing to their unique structural features, isothiocyanates (ITCs) are a class of highly useful and inimitable reagents as the N=C=S group serves both as electrophile and nucleophile in organic...
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Synthesis of Deuteriodifluoromethylthiolated Isocoumarins-1- imines and Isocoumarins Enabled by Multi-Component Reagents System (MCRS)

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00328D, Communication
Xuemin Li, Haofeng Shi, Jiaxin He, Jialiang Wu, Fengxia Sun, Yunfei Du
The combining use of BnSCF2D, mCPBA and Tf2O serves as an efficient multi-component reagents system (MCRS) for the synthesis of deuteriodifluoromethylthiolated isocoumarins-1-imines/isocoumarins via intramolecular cyclization/ deuteriodifluoromethylthiolation of 2-alkynylbenzamide/2-alkynylbenzoates. The approach...
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Natural products from human microbiome: an emergent frontier in organic synthesis and drug discovery

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00236A, Review Article
Goverdhan Mehta, Saumitra Sengupta, Srihari Pabbaraja
Often referred to as “second genome”, human microbiome is at the epicenter of a complex inter-habitat biochemical network, such as the “gut-brain axis”, which have emerged as significant determinant of...
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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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Design, synthesis, and biological application of A–D–A-type boranil fluorescent dyes

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00297K, Paper
Wei Luo, Yiling Li, Liang Wang, Yanhua Qin, Qiao Cheng, Guochang Hu, Chaoyi Yao, Xiangzhi Song
Acceptor–donor–acceptor boranil fluorescent dyes, CSU-BF-R (R = H, CH3, and OCH3), were developed with strong red fluorescence and large Stokes shifts. CSU-BF-OCH3 could selectively sense intracellular hypochlorous acid in living cells and zebrafish.
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Measuring local pH at interfaces from molecular tumbling: A concept for designing EPR-active pH-sensitive labels and probes

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00167B, Paper
Open Access
Maxim A. Voinov, Nicholas Nunn, Roshan Rana, Atli Davidsson, Alex I. Smirnov, Tatyana I. Smirnova
EPR-based local pH measurements based on changes in rotational dynamics of spin-bearing molecules upon protonation.
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Facile synthesis of tetrahydroquinoline containing dithiocarbamate derivatives via one-pot sequential multicomponent reaction

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00490F, Communication
SIDDHARTHA KUMAR SENAPATI, Anit Pal, Animesh Das
An efficient sequential multi-component method for the synthesis of tertrahydroquinoline containing dithiocarbamate has been developed. This reaction involved a boronic acid-catalyzed reduction of quinoline to tertrahydroquinoline, followed by nucleophilic addition...
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Regioselective synthesis of 4-arylamino-1,2-naphthoquinones in eutectogel as a confined reaction medium using LED light

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00140K, Communication
R. Vara Prasad, Yogendra Kumar, R. Arun Kumar, Tohira Banoo, Subbiah Nagarajan
The use of a simple carbohydrate-derived eutectogel facilitating a LED-light-induced regioselective synthesis of 4-arylamino-1,2-naphthoquinones in good yields is reported.
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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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Efficient synthesis of SCF3-containing 3-alkenylquinoxalinones via three-component radical cascade reaction

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00363B, Paper
Si-Yu Wang, Chu Liu, Wei Yang, Zhong-Ying Tian, Lin Yuan, Long-Yong Xie
A three-component cascade reaction of quinoxalinones, alkynes and AgSCF3 toward complete E-selective SCF3-containing 3-alkenylquinoxalinones was developed.
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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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K2CO3-Mediated (3+3-1) Annulation of 1,3-Acetonedicarboxylates with 2-Fluoro-1-nitroarenes: Synthesis of Indoles

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00488D, Paper
Meng-Yang Chang, Chin-Huey Ho, Hsing-Yin Chen
The K2CO3-mediated one-pot reaction of 1,3-acetonedicarboxylates with 2 equiv. of substituted 2-fluoro-1-nitrobenzenes has been developed to synthesize various 2,3-dicarboxylate indoles via a tandem (3 + 3 − 1) annulation pathway....
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Built-in Browser Support for Responsive Images

Take advantage of the new element and new features of in your next responsive website.




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The EME Logger extension




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IFSC: Aircraft leasing gets a big boost

Around 80 per cent of the total commercial fleet in India is leased against 53 per cent of the same, globally




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Lost your baggage in transit? You might find it in Alabama

Every year, nearly 25 million bags are lost in transit out of 4.3 billion 




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Next order of business for Tata Sons

How will Tata Sons turn around all the airlines under its fold, except maybe the Kochi-based Air India Express?




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Deep diving into design philosophies

Airbus and Boeing differ in their approach to automation




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Decarbonising flying

IATA shares proposes 65 per cent of aviation-emitted carbon will be abated through sustainable aviation fuel




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Redressing flaws: IndiGo needs to tweak its way

How the human element can help the airline appease passengers and employees




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Yoke vs. sidestick: Jury still out on what works best for pilots

Why do Airbus commercial aircraft have sidesticks and Boeing have yokes as control units?




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Cabin crew with an invisible cape 

Being a cabin crew member is not a mere job, but an ineffable life experience




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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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Why opening the emergency door mid-flight is not possible




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Reviving businesses will benefit from air cargo’s growth

India’s air cargo industry is well positioned to scale up further, thanks to a strong airport cargo infrastructure




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Hong Kong unveils responsible AI framework for financial sector

Hong Kong’s responsible AI framework comes amid increasing international competition and tensions affecting access to AI technology




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OpenAI chair's AI startup Sierra gets $4.5 billion valuation in latest funding round

One-year-old Sierra focuses on selling artificial intelligence-powered customer service chatbots to enterprises