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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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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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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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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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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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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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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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Exploring the mechanism of the reductive amination of acetophenones via Borch approach: the role of the acid catalyst

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00160E, Paper
João Pedro Albuquerque Souza, Amanda Krauskopf Jacobs, Leandro Piovan, Renan Borsoi Campos
The energetic viability of several mechanistic variations of the reductive amination of acetophenones via the Borch approach was reexamined through density functional theory calculations. The crucial involvement of the acid...
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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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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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Discovery of selective monosaccharide receptors via dynamic combinatorial chemistry

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00015C, Communication
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Miguel Alena-Rodriguez, Marcos Fernandez-Villamarin, Ignacio Alfonso, Paula M. Mendes
An effective workflow to discover selective saccharide receptors by combining dynamic combinatorial chemistry with isothermal titration calorimetry and NMR.
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TEMPO/PhI(OAc)2 promotes the α-aminophosphinoylation of alcohols with amines and H-phosphine oxides in aqueous medium

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00302K, Communication
Qiang Huang, Xin Jin, Lvjia Wu, Jiangdong Li, Qianlu Xing, Xianheng Wang, Changkuo Zhao
The aminophosphinoylation of alcohols with amines and H-phosphine oxides provides an efficient and mild approach to access various α-aminoalkylphosphine oxides in good yields with good tolerance of functional groups using H2O as a clean solvent.
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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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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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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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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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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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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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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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Updates to the service worker cache API




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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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Pandemic: Contactless technology on an overdrive

As demand for travel rises, industry must meet it while ensuring passenger safety




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Those magnificent flying machines

The aviation industry’s roller-coaster ride




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Making a comeback

The aviation industry has proved its resilience by standing strong, despite an unprecedented economic crisis




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No turning back

If no action is taken, aviation’s contribution towards greenhouse gas emissions will increase




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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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The art of avoiding accidents in air

Flying distance may vary based on flight phases, altitudes and regions




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Embraer expects capacity dynamics to tilt demand in its favour

The plane maker’s current foray attempts to shed the tentativeness that overshadowed its earlier endeavours




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Apple AirPods Pro’s new hearing aid feature could help people face a problem they’d rather ignore

Millions who could benefit from hearing aids have never tried them, but the Apple AirPods could change this




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Google’s moneymaking machine still pumping out massive profits despite multiple threats

Google is still thriving while the company navigates through a pivotal shift to artificial intelligence and battles regulators trying to topple its internet empire




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OpenAI builds first chip with Broadcom and TSMC, scales back foundry ambition

OpenAI is working with Broadcom and TSMC to build its first in-house chip designed to support its artificial intelligence systems, per sources




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Crypto firm Consensys to cut 20% of workforce amid macroeconomic, regulatory headwinds

The crypto firm added that elevated interest rates, inflationary pressures, and tightening liquidity have created a more “cautious macroeconomic environment”




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Chinese researchers develop AI model for military use on back of Meta's Llama

ChatBIT was fine-tuned and "optimised for dialogue and question-answering tasks in the military field", the paper said




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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 […]




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WHO to evacuate 1,000 Gazan women, children for urgent medical care

Last week, U.N. investigators said Israel was deliberately targeting health facilities in Gaza, and killing and torturing medical personnel there, accusing the country of "crimes against humanity".




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Dietary restriction or good genes: new study tries to unpack which has greater impact on lifespan

If we know that genetics and lifestyle affect how long you live, which one is more important? And how do they interact?




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High cataract rate among elderly in Mucherla, Meerkhanpet of Rangareddy district, says survey

HHF’s screening of 200 patients in Mucherla and Meerkhanpet found that 21% had senile cataracts, 18% had immature cataracts, and 15% had refractive errors




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Rapid assessment of pulse polio campaign shows high vaccine coverage, highlights gaps in Chennai

Chennai accounted for nearly 21% of the non-vaccinated children, highlighting the gaps in an urban area and the need for targeted community outreach




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Acute Flaccid Paralysis surveillance as a crucial defence against polio in India | Explained

India needs to continue efforts to maintain its polio-free status, and AFP surveillance has to remain a cornerstone of its strategy




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Over 77 per cent of India’s children lack WHO-suggested diversity in diet, study finds

The states of Uttar Pradesh, Rajasthan, Gujarat, Maharashtra and Madhya Pradesh reported the highest levels of inadequate diversity in children's diets -- all above 80 per cent -- while Sikkim and Meghalaya were the only two to report an under-50 per cent prevalence




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WHO says ‘intense bombardment’ halts Gaza polio vaccinations

The U.N. health body said it had been “compelled to postpone” the bid to give 119,279 children in northern Gaza a second vaccine dose due to the escalating violence




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Trachoma eliminated as a public health problem in India; what next?

The achievement marks a significant public health victory and has profound economic implications. Trachoma’s impact, through blindness and visual impairment, results in an estimated economic loss of $2.9 to 5.3 billion annually due to reduced productivity




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Drugs regulator finds 49 samples not of standard quality, manufacturers asked to withdraw their products

Four spurious drugs were also found and action has been initiated against the makers, the DCGI said