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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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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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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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Identification and quantification of local antiaromaticity in polycyclic aromatic hydrocarbons (PAHs) based on the magnetic criterion

Org. Biomol. Chem., 2024, 22,3035-3044
DOI: 10.1039/D4OB00114A, Paper
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Erich Kleinpeter, Andreas Koch
The ring current effect of entirely and partly (anti)aromatic PCHs are calculated and employed to visualize, qualify and quantify existing (anti)aromaticity, especially to decide unequivocally between PAHs and PAAHs.
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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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Direct access to pyrrole anhydrides via oxidative self-coupling of pyrrole carboxaldehydes

Org. Biomol. Chem., 2024, 22,3045-3052
DOI: 10.1039/D4OB00052H, Paper
Surabhi Panday, Tapas Maity, Pratibha Bhatti, Joydev K. Laha
An elegant synthesis of pyrrole-2-carboxylic acid anhydrides from pyrrole-2-carboxaldehydes using TBAI as a catalyst and tert-butyl hydroperoxide (TBHP) as an oxidant is described herein.
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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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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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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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Dess–Martin periodinane-mediated oxidation of the primary alcohol of cytidine into a carboxylic acid

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00240G, Communication
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Alexandra R. E. Serre, Vibhu Jha, Adèle Rivault, Leif A. Eriksson, Goreti Ribeiro Morais, Robert A. Falconer
Herein we describe the first example of the conversion of the primary alcohol of cytidine into a carboxylic acid by use of the Dess–Martin periodinane oxidising agent.
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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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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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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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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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Rolling out Public Key Pinning with HPKP Reporting




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Wanted: A booster dose for airlines

As vaccination numbers increase, airlines and the government look for the middle path to revive the beleagured travel sector




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A lift for MRO

It is time to help Indian aviation’s technical side realise its potential




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Year-end blues for beleagued airlines

The results of IndiGo and SpiceJet hold clues to the mid-term future of the country’s airline industry




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As the price of aviation turbine fuel soars, airlines’ finances spin out of control




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Regional airlines fly into rough weather

From poor applicability of policy to lack of quality manpower and capital, problems plaguing them are manifold




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The making of ‘agile’ airlines

How adoption of AI, ML can empower flying




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Domestic air travel leads airline recovery: Boeing

Low-cost carriers aid market with point-to-point structure and affordable rates




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Reskilling of airline workforce needed

Industry grapples with skilling/reskilling employees right from pilots to ground handling staff whose skills may be redundant




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Greenfield airports on a slippery runway

The success of these new airports is contingent on the ability to attract international traffic




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A frequent flier’s tip on flying

Covid tip: pick the last seat because “nobody coughs backwards”




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Omicron: Airlines on a wing and prayer

Over 3,000 flights were cancelled on the eve of Christmas and cancellations are expected to double as New Year approaches




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2022 holds promise for the airline sector

Omicron might dent growth, but the long-term outlook seems promising




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Demand for more flight schools soars

Pilot shortage is hurting airline operations in India, with the industry expected to need at least 1,000 to 1,500 pilots every year




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Robust flight plans can keep airlines afloat




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Deep tech is helping airlines sustain operations during Covid

Integrated biometric-enabled frameworks for real-time test results, travel details and vaccine status are key to making air travel safe




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Breaking down airline engineering and maintenance

An aircraft has three critical phases; induction, in-service and redelivery




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From geopolitics strife to a war of words between two aviation giants

Qatar Airways and Airbus lock horns over safety concerns




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Another tough year for airlines

Ukraine-Russia conflict to result in the steep escalation of aircraft leasing charges




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Short-haul flights redefining air travel

 While the growth of international flights remains muted, demand for narrow-bodied aircraft witnesses a renewed surge 




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Corporate travel is unlikely to reach pre-Covid levels

However, with offices opening up, many airlines are seeing increased demand with an uptick for premium cabins




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Domestic airline industry may face a rejig

The pandemic laid bare fault-lines within India’s airlines




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Electric aircraft set to transform urban mobility 

Investors are pouring in billions of dollars into eVTOL project (electric vertical take offs and landing aircraft) to ferry passengers