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Divergent syntheses of okaramines C, J, L, and S-U

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00587H, Communication
Xiao Wan Li, Tong xu Si, Ya-Ping Liu, Mingzhong Wang, Albert S. C. Chan
The total synthesis of six novel okaramines (C, J, L, and S-U) was accomplished with a precise synthesis scheme involving few steps and with practical yield of 6.7%-23.0%. The significance...
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Synthesis of unsymmetrical benzils via palladium-catalysed α-arylation–oxidation of 2-hydroxyacetophenones with aryl bromides

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00575D, Paper
Open Access
Takanori Matsuda, Souta Oyama
Unsymmetrical benzils are synthesised by a one-pot tandem palladium-catalysed α-arylation and oxidation of 2-hydroxyacetophenones with aryl bromides.
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Enantioselective Synthesis of Indanone Spiro-Isochromanone Derivatives via Dinuclear Zinc-Catalyzed Michael/Transesterification Tandem Reaction

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00541J, Paper
Xiao-Chao Yang, Meng Xu, Jin-Bao Wang, Meng-Meng Liu, Francois Mathey, Yuan-Zhao Hua, Mincan Wang
An enantioselective Michael/transesterification tandem reaction of α-hydroxy indanones with ortho-ester chalcones was realized by dinuclear zinc catalysts. A series of enantiomerically pure spiro[indanone-2,3’-isochromane-1-one] derivatives were obtained in good yields with...
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Insights into the secondary structures of lactam N-substituted stapled peptides

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00767F, Communication
Aldrin Vasco Vidal, Celia Gonzalez, Stefan Gröger, W Brandt, Jochen Balbach, Carlos Perez, Ludger A. Wessjohann, Daniel G. Rivera
Stapled peptides derived from the Ugi macrocyclization comprise a special class of cyclopeptides with an N-substituted lactam bridge cross-linking two amino acid side chains. Herein we report a comprehensive analysis...
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Protein labeling approach to improve lysosomal targeting and efficacy of antibody–drug conjugates

Org. Biomol. Chem., 2020, 18,3229-3233
DOI: 10.1039/D0OB00265H, Communication
Ying Han, Yifan Da, Mingjia Yu, Yaping Cheng, Xin Wang, Jiale Xiong, Guoying Guo, Yan Li, Xianxing Jiang, Xiaoqing Cai
An anti-EGFR nanobody was labeled at the C-terminus with a lysosome-sorting NPGY (Asn-Pro-Gly-Tyr) motif via sortase-mediated ligation to enhance the clathrin-mediated endocytosis.
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Targeting STAT3 anti-apoptosis pathways with organic and hybrid organic–inorganic inhibitors

Org. Biomol. Chem., 2020, 18,3288-3296
DOI: 10.1039/C9OB02682G, Paper
Matthew B. Minus, Haopei Wang, Jaime O. Munoz, Alexandra M. Stevens, Alicia E. Mangubat-Medina, Michael J. Krueger, Wei Liu, Moses M. Kasembeli, Julian C. Cooper, Mikhail I. Kolosov, David J. Tweardy, Michele S. Redell, Zachary T. Ball
Recurrence and drug resistance are major challenges in the treatment of acute myeloid leukemia (AML) that spur efforts to identify new clinical targets and active agents.
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The quasi-irreversible inactivation of cytochrome P450 enzymes by paroxetine: a computational approach

Org. Biomol. Chem., 2020, 18,3334-3345
DOI: 10.1039/D0OB00529K, Paper
Emadeldin M. Kamel, Al Mokhtar Lamsabhi
The potency of paroxetine as a P450 inhibitor is mainly attributed to the availability of two active sites on its structure, its compatibility with P450's active site and the ease of its tight coordination to heme iron.
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Direct recognition and sensitive detection of circular RNA with ligation-based PCR

Org. Biomol. Chem., 2020, 18,3269-3273
DOI: 10.1039/D0OB00625D, Communication
Pengbo Zhang, Na Guo, Kejian Gao, Fengxia Su, Fangfang Wang, Zhengping Li
A sensitive and specific method for circRNA detection is developed through the direct ligation of two ingeniously designed DNA probes.
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Visible light induced 3-position-selective addition of arylpropiolic acids with ethers via C(sp3)–H functionalization

Org. Biomol. Chem., 2020, 18,3258-3262
DOI: 10.1039/D0OB00480D, Communication
Zi-juan Wan, Xiao-feng Yuan, Jun Luo
Although the 2-position-selective decarboxylative coupling or addition of arylpropiolic acids with cyclic ethers has been intensively investigated, selective functionalization of arylpropiolic acids at the 3-position is still a big challenge.
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Modular continuous flow synthesis of orthogonally protected 6-deoxy glucose glycals

Org. Biomol. Chem., 2020, 18,3254-3257
DOI: 10.1039/D0OB00522C, Communication
Subbarao Yalamanchili, Tu-Anh V. Nguyen, Nicola L. B. Pohl, Clay S. Bennett
The use of a continuous flow platform for the rapid and highly efficient construction of differentially protected glycals from commercial sources is described.
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A visible-light-induced “on–off” one-pot synthesis of 3-arylacetylene coumarins with AIE properties

Org. Biomol. Chem., 2020, 18,3346-3353
DOI: 10.1039/D0OB00479K, Paper
Xinjie Wu, Ming Jia, Mengmeng Huang, Jung Keun Kim, Zheng Zhao, Junkai Liu, Jinhu Xi, Yabo Li, Yangjie Wu
A mild one-pot approach to 3-arylacetylene coumarins with potential AIE activities was developed via photosensitizer-free photocatalysis and thermocatalysis.
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Base-promoted 1,6-conjugate addition of alkylazaarenes to para-quinone methides

Org. Biomol. Chem., 2020, 18,3354-3359
DOI: 10.1039/D0OB00419G, Paper
Amritha Rayaroth, Rajat Kumar Singh, Kalyanakrishnan A. V., Krishna Hari, Alagiri Kaliyamoorthy
1,1,2-Triarylethanes embedded with an azaarene unit were prepared in a single step at ambient temperature via the sodium hexamethyldisilazide mediated 1,6-conjugate addition of unactivated alkylazaarenes on para-quinone methides (p-QMs).
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Modular synthesis of oligoacetylacetones via site-selective silylation of acetylacetone derivatives

Org. Biomol. Chem., 2020, 18,3297-3302
DOI: 10.1039/D0OB00501K, Paper
Parantap Sarkar, Yuya Inaba, Hayato Shirakura, Tomoki Yoneda, Yasuhide Inokuma
Aliphatic oligoketones with tailored carbonyl and substituent sequences were modularly synthesized utilizing site-selective formation of enol silyl ethers. Their unique conformational preferences in solid-state were revealed by X-ray crystallography.
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Copper-catalyzed direct amination of benzylic hydrocarbons and inactive aliphatic alkanes with arylamines

Org. Biomol. Chem., 2020, 18,3263-3268
DOI: 10.1039/D0OB00491J, Communication
Hua Yao, Bo Xie, Xiaoyang Zhong, Shengzhou Jin, Sen Lin, Zhaohua Yan
A new synthetic method toward direct C–N bond formation through saturated C–H amination of benzylic hydrocarbons and inactive aliphatic alkanes with primary aromatic amines under an inexpensive catalyst/oxidant (Cu/DTBP) system has been developed.
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KI/TBHP-promoted [3 + 2] cycloaddition of pyrrolo[1,2-a]quinoxalines and N-arylsulfonylhydrazones

Org. Biomol. Chem., 2020, 18,3360-3366
DOI: 10.1039/D0OB00494D, Paper
Zhen Yang, Jing He, Yueting Wei, Weiwei Li, Ping Liu
A series of diverse fused [1,2,4]triazolo[3,4-c]quinoxalines was obtained by an efficient KI/TBHP-promoted [3 + 2] cycloaddition of pyrrolo[1,2-a]quinoxalines and N-arylsulfonylhydrazones.
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Dipyrazolodioxadiazocines as shelf-stable “ready-to-use” precursors for an in situ generation of enolate-iminium 1,4-dipoles: a straightforward atom-economical approach to pyrazolo[5,1-d][1,3,5]dioxazines

Org. Biomol. Chem., 2020, 18,3382-3391
DOI: 10.1039/D0OB00451K, Paper
Vladimir E. Zhulanov, Valeria A. Vigovskaya, Maksim V. Dmitriev, Pavel S. Silaichev, Andrey N. Maslivets, Michael Rubin
Generation of cyclic enolate-iminium 1,4-dipoles via thermolysis of dipyrazolodioxadiazocines in the presence of ketones allowed for efficient preparation of pyrazolo[5,1-d][1,3,5]dioxazines.
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Controlling the liberation rate of the in situ release of a chemical fuel for the operationally autonomous motions of molecular machines

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00669F, Paper
Chiara Biagini, Giorgio Capocasa, Daniele Del Giudice, Valerio Cataldi, Luigi Mandolini, Stefano Di Stefano
Aminolysis of the anhydride of 2-cyano-2-phenylpropanoic acid can be employed to conveniently regulate the liberation rate of the related acid which, in turn, can be used as a fuel for acid–base operated molecular machines.
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Late-stage synthesis and application of photoreactive probes derived from direct benzoylation of heteroaromatic C–H bonds

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00336K, Communication
Kevin D. Hesp, Jun Xiao, Graham M. West
A synthetically-driven, late-stage C–H benzoylation strategy for the expedited preparation and evaluation of heterocyclic alternatives to more classical benzophenone photoreactive probes is reported.
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Arylation of Indoles Using Cyclohexanones Dually-Catalyzed by Niobic Acid and Palladium-on-Carbons

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00702A, Paper
Kazuho Ban, Yuta Yamamoto, Hironao Sajiki, Yoshinari Sawama
3-Arylindoles were easily constructed from indoles and cyclohexanone derivatives using a combination of catalytic niobic acid-on-carbon (Nb2O5/C) and palladium-on-carbon (Pd/C) under heating conditions without any oxidants. The Lewis acidic Nb2O5/C...
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Hierarchical Self-Assembly of Azobenzene Dyad with Inverted Amide Connection into Toroidal and Tubular Nanostructures

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00833H, Communication
Shiki Yagai, Takuho Saito
Inversion of the connectivity of amide groups in foldable azobenzene dyads with chiral side chains, which can self-assemble into toroids and nanotubes, significantly increases the thermal stability of these aggregates....
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Efficient synthesis of a galectin inhibitor clinical candidate (TD139) using a Payne rearrangement/azidation reaction cascade

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00910E, Paper
Jacob St-Gelais, Vincent Denavit, Denis Giguère
Selective galectin inhibitors are valuable research tools and could also be used as drug candidates. In that context, TD139, a thiodigalactoside galectin-3 inhibitor, is currently being evaluated clinically for the...
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Man arrested for molesting Finnish woman in Jaipur

A person has been arrested in Jaipur for allegedly robbing and molesting a Finnish woman at a bar cum restaurant, police said.




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Fire arm, opening an eatery: get licence application forms online

Now, getting a licence for a fire-arm or operating an eatery will be easy with Delhi Police on Tuesday launching a dedicated website for its Licencing Branch.




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70 per cent of teachers in Delhi schools are obese: survey

Nearly 70 per cent of schoolteachers in the national capital are overweight and obese, a recent survey has claimed.




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Aspiring actor-cum-model arrested for killing IT professional

A 20-year-old aspiring actor- cum-model was arrested in the national capital for allegedly murdering a young woman IT professional a week ago after she refused to heed to his demand for money.




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Mumbaikars usher in Ganesh amidst flu scare

Terror alerts and swine flu scare did not dampen the spirit of Mumbaikars as they welcomed the elephant headed-god.




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Five-year-old survives 40-feet fall with minor scratches

A five-year old boy here survived a 40-feet fall from a multi-storeyed building with minor scratches.




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'I'd have done anything else other than write this book': Akhil Sharma

New York-based writer Akhil Sharma 's novel Family Life has received rave reviews. The autobiographical book traces the journey of a family that moves to the US from India, its eldest son suddenly suffering a freak accident.




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'In Nepal, some street children are controlled by gangs'

An unwanted child, a street urchin, a knife-wielding gang member and a child labourer — Basu Rai endured the vicissitudes of fate. But after his rescue and rehab, he dedicated his life to saving other street children.




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Pak politicians want to resolve Kashmir — military won't allow this: Arif Jamal

Arif Jamal is a Pakistani journalist and South Asia expert based in America.




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​'Advertising's art of persuasion — political ads will grow': Prasoon Joshi

Author and advertising authority headed the Titanium Lions jury at 2014's Cannes International Advertising Festival.




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Women suffer sanitation absence most — also impacts economy: Bindeshwar Pathak

One month after the horrific Badaun gang rape exposed how gravely at risk women and minors lacking domestic toilets are.




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Australia-India cricket rivalry has even bettered Ashes: John Harnden

CEO of the ICC World Cup 2015 John Harnden spoke with Amin Ali about ensuring excitement in cricket's mega-tournament, clamping down on racism, managing 'minnows' matches — and how Australia is sizing up India as a rival for the trophy.




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Swiss accounts are a diversion. Bulk of black money is right here in India

The scent of 'black money' is in the air again. At the Supreme Court's order, Modi sarkar has set up a Special Investigation Team to look into cases of illegal outflow of money to foreign havens.




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Singapore appoints Sikh as Army chief

Singapore has appointed Brigadier General Ravinder Singh as its next army chief, the first Sikh in nearly 30 years to be given the force's baton.




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Hindu guru gets 14 years prison for sexual molestation in US

Absconding Indian godman Prakashanand Saraswati, also known as Shree Swamiji, has been sentenced to 14 years in prison and fined USD 10,000.




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NRI dentist in UK faces charges of seducing patient

An NRI dentist, once the face of Oral B toothpaste and appears on a British TV show, has been accused of seducing a patient on the couch of his dental clinic and marital home, a disciplinary hearing was told.




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Five-year-old Indian becomes millionaire

A five-year-old Indian boy has become a millionaire overnight after winning a lottery at a national bond draw here.




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Australia's Victoria police inducts first turban wearing Sikh

Police in Australia's Victoria state today inducted its first officer from Sikh community who will wear a newly designed police turban, a media report said today.




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Gujarati icing on Will-Kat wedding cake!

The royal wedding cake is set to have a Gujarati connection. It has emerged that Prince William and Kate Middleton have chosen a cake company run by a Gujarati in Leicestershire.




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Lucknow zoo animals are more active in lockdown




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Kanpur baraat stuck in Bihar for 45 days

Khushbu Khatoon of Begusarai in Bihar was a happy bride after her nikah was solemnised with Kanpur's Imtiyaz on March 21.




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Two more areas turn hotspots after 3 test +ve




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Covid warriors in Lucknow put duty before family




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UP: 63 flee quarantine centre, all traced




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UP: Heritage tag for 100-year-old trees




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Maharashtra: Major train accident averted on Urali-Loni route

The driver applied the emergency brakes after spotting around 20 people, including women sitting on a track, and some of them even walking with their luggage on the tracks.




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Delhi govt says it will pay train fare of migrants

Delhi government on Friday said it would bear the cost of train travel of migrant workers if their home states didn’t respond on the issue.




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Funds for salaries late, inadequate: DU colleges

For the second time this year, Delhi government has allegedly released inadequate funds for the salaries of teaching and non-teaching staff of 12 Delhi University colleges, that too after a month-long delay.




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Tears of relief at IGI arrival and departure

At 12.05pm on Friday, Air India flight AI-381 made a smooth landing at Indira Gandhi International Airport. Though half an hour late in arriving, the 234 passengers from Singapore were delighted to step on home soil after two months of anxiety and uncertainty. Their relatives weren’t allowed to meet them, and yet the relief of being back in India made them grin, wave their hands and give the thumbs up sign.