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Synthesis of Asp-based lactam cyclic peptides using an amide-bonded diaminodiacid to prevent aspartimide formation

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00472H, Communication
Wen-Jie Li, Jun-You Chen, Hui-Xia Zhu, Yi-Ming Li, Yang Xu
A diaminodiacid (DADA) containing an amide bond can be used in Fmoc solid-phase peptide synthesis (SPPS) of an Asp-based lactam cyclic peptide with no aspartimide formation.
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Asymmetric total synthesis of humulane sesquiterpenoids alashanoids B, C, E, and F and 2,9-humuladien-6-ol-8-one

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00393D, Paper
Rasmita Barik, Samik Nanda
Naturally occurring sesquiterpenes having humulane frameworks are structurally intriguing and possess significant biological profiles.
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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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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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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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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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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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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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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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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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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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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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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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How long do commercial aircraft last?

What airlines can do to extend the longevity of their fleet




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




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‘The challenge was in getting the aircraft’s custom clearance’

Private jet operator JetSetGo’s CEO Kanika Tekriwal describes the intricacies of directly importing and leasing an aircraft




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Gearing up to fly twice as fast as sound

The US-based start-up Boom Supersonic is putting together an aircraft that can fly at a maximum speed of Mach 2.2




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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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A380: How Airbus forecast misfired

Sinks $25 billion in the process




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As India builds its newest airports, it needs robust, fail-proof SOPs

A near air mishap on Bengaluru skies that put the lives of 430 people in danger shows safety risk norms require constant refresh




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In case the engine gives out

If an aircraft’s engine fails, the pilot has nearly half an hour to find a landing spot




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Will Akasa Air’s contra bet on Boeing 737 Max instead of Airbus pay off?

Rakesh Jhunjhunwala’s Akasa airline has gone against the tide, placing its bets on Boeing aircrafts; it now needs to carve out a niche for itself 




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Air infrastructure plans should be future-proof

India’s aviation story is full of delayed, untapped and under-utilised potential




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Why do plane crashes happen?




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Post-pandemic, OTAs are coming of age

Are they finally paying up or paying off?




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Why has private capital not been taken to Indian aviation 

With banks becoming increasingly cautious and credit flows tightening, private capital must be explored and enticed




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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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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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ChatGPT will now work as a search engine as OpenAI partners with some news outlets

OpenAI is launching a ChatGPT-powered search engine that could put the artificial intelligence company in direct competition with search giant Google




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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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Transformation Stories #4 A New Podcast Interview With Me (Rob Larsen)

Check out yours truly on an episode of Atlas Systems’ Transformation Stories. A hands-on leader and change-maker with 20 years of experience, Rob Larsen remains at the forefront of software-led innovation – in financial services and the larger enterprise world. In this all-new conversation with Atlas Systems, Larsen offers insights into finding the right pace […]




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HTML5 Boilerplate 9.0.1 Released

See it on GitHub! View it on npm! This release was kicked off because of Gulp 5. Gulp 5 has breaking changes so we had to work through the upgrade manually. In the process of doing that upgrade we discovered a couple of bugs. Christian Oliff noticed that tests were failing on Windows I noticed […]




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Out-of-pocket expenditure on health in Kerala is highest in country despite increased State investments

National Health Accounts figures show the per capita out-of-pocket expenditure on health in Kerala stands at ₹7,889. However, Kerala also tops the list when it comes to the per capita government spending on health, at ₹4,338




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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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WHO certifies Egypt as malaria-free; calls it ‘historic feat’ ending ancient scourge

Globally, 44 countries and one territory have now been certified as malaria-free




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Sexual harassment rampant in Maharashtra medical colleges, finds survey

The survey also found that a majority of students believed that reporting these events could negatively affect their grades and future prospects; it highlighted the need for better safety mechanisms on campus




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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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Rajasthan-based firm barred from making ‘Insulin’ homeopathic tablets

A licence for the manufacture of this product was cancelled; this follows a complaint from Kerala-based RTI activist K.V. Babu with the Prime Minister’s public grievance cell




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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




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$25-million Pandemic Fund aims to curb ‘zoonotic’ diseases

The Centre will implement the G20 Pandemic Fund, which is aimed at enhancing the country’s “animal health security”, in partnership with the Asian Development Bank (ADB), the World Bank and the Food and Agriculture Organization (FAO).




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Tuberculosis infected 8 million people last year, the most WHO has ever tracked

The World Health Organization says more than 8 million people were diagnosed with tuberculosis last year




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As breast cancer incidence rises, doctors raise importance of early detection, need for women to be breast aware

Chennai accounts for highest crude incidence rate of breast cancer in T.N., data shows; a number of factors have led to this, say doctors




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What is breast density and how is it associated with cancer? Explained

Breast density matters because of two main reasons: it may make it harder to detect signs of cancer on a mammogram, and it is linked with an increased risk of breast cancer