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Three-component synthesis of 1,4-benzothiazines via iodide-catalyzed aerobic C–H sulfuration with elemental sulfur

Org. Biomol. Chem., 2020, 18,3234-3238
DOI: 10.1039/D0OB00074D, Communication
Jingjing Jiang, Xiaolong Tuo, Zhuquan Fu, Huawen Huang, Guo-Jun Deng
Five to Six: Beyond the well-established thiazole formation from elemental sulfur, this method provides the first access to the corresponding six-membered N,S-heterocyclic products via direct functionalization of multiple C–H bonds.
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Phenylboronic acid-catalyzed tandem construction of S–S and C–S bonds: a new method for the synthesis of benzyl disulfanylsulfone derivatives from S-benzyl thiosulfonates

Org. Biomol. Chem., 2020, 18,3243-3248
DOI: 10.1039/D0OB00442A, Communication
Raju Jannapu Reddy, Md. Waheed, Gamidi Rama Krishna
A novel and unique phenylboronic acid-catalyzed tandem construction of S–S and C–S bonds via dimerization–sulfonylation has been disclosed for the synthesis of benzyl disulfanylsulfone derivatives.
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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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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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Synthesis of α-CF3-substituted E-dehydroornithine derivatives via copper(I)-catalyzed hydroamination of allenes

Org. Biomol. Chem., 2020, 18,3274-3280
DOI: 10.1039/D0OB00580K, Paper
Anna N. Philippova, Daria V. Vorobyeva, Florian Monnier, Sergey N. Osipov
Novel α-CF3-substituted E-dehydroornithine derivatives have been synthesized via the Cu(I)-catalyzed hydroamination of α-CF3-α-allenyl-α-aminocarboxylates/phosphonates with different amines.
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Chemo- and regioselective click reactions through nickel-catalyzed azide–alkyne cycloaddition

Org. Biomol. Chem., 2020, 18,3374-3381
DOI: 10.1039/D0OB00579G, Paper
Woo Gyum Kim, Seung-yeol Baek, Seo Yeong Jeong, Dongsik Nam, Ji Hwan Jeon, Wonyoung Choe, Mu-Hyun Baik, Sung You Hong
Nickel-catalyzed [3 + 2] cycloaddition reactions of unsymmetrical alkynes and organic azides afford substituted 1,2,3-triazoles with high levels of chemo- and regioselectivity.
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Chiral bifunctional sulfide-catalyzed asymmetric bromoaminocyclizations

Org. Biomol. Chem., 2020, 18,3367-3373
DOI: 10.1039/D0OB00459F, Paper
Takumi Nakamura, Ken Okuno, Kazuma Kaneko, Masahiro Yamanaka, Seiji Shirakawa
A chiral bifunctional sulfide catalyst bearing a urea moiety promotes the enantioselective bromoaminocyclization of 2-allylanilines to produce optically active 2-substituted indolines.
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O-Cyclopropyl hydroxylamines: gram-scale synthesis and utility as precursors for N-heterocycles

Org. Biomol. Chem., 2020, 18,3281-3287
DOI: 10.1039/D0OB00611D, Paper
Kaitlyn Lovato, Urmibhusan Bhakta, Yi Pin Ng, László Kürti
A novel and scalable synthesis of O-cyclopropyl hydroxylamines is reported. These compounds are bench-stable and have been shown to be practical precursors for the synthesis of N-heterocycles via a di-heteroatom [3,3]-sigmatropic rearrangement.
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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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Gold(III)-catalyzed azide-yne cyclization/O–H insertion cascade reaction for the expeditious construction of 3-alkoxy-4-quinolinone frameworks

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00745E, Paper
Jingjing Huang, Han Su, Ming Bao, Lihua Qiu, Yuanqing Zhang, Xinfang Xu
A gold-catalyzed cascade reaction has been developed, and it provides an expeditious access to 3-alkoxy-4-quinolines and applications in alkaloid synthesis.
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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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Spiroconyone A, a new phytosterol with a spiro [5,6] ring system from Conyza japonica

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00666A, Paper
Long-Gao Xiao, Yu Zhang, Hong-Li Zhang, Ding Li, Qiong Gu, Gui-Hua Tang, Qian Yu, Lin-Kun An
The first rearranged phytosterol (spiroconyone A) with an unusual spiro [5,6] ring system and two new TDP1 inhibitors 7 and 10 showing a strong synergistic effect with topotecan were isolated from Conyza japonica.
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Synthesis of gem-difluoroalkenes via nickel-catalyzed allylic defluorinative reductive cross-coupling of trifluoromethyl alkenes with epoxides

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00535E, Communication
Xiao-Yu Lu, Run-Chuang Jiang, Jia-Mei Li, Chuang-Chuang Liu, Qing-Qing Wang, Hai-Pin Zhou
A nickel-catalyzed defluorinative reductive cross-coupling of trifluoromethyl alkenes with epoxides has been developed.
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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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Correction: Nickel-catalyzed cyanation of phenol derivatives activated by 2,4,6-trichloro-1,3,5-triazine

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB90052D, Correction
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Liang Wang, Yaoyao Wang, Jun Shen, Qun Chen, Ming-Yang He
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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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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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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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Climbing Everest, I've proved a tribal girl can do something: Malavath Poorna

At just 13 years, Malavath Poorna from Telangana has become the youngest female climber in the world to scale Mount Everest. Speaking with Rohit E David, Poorna discussed how she has emerged from a family of agricultural labourers to become a mountaineer, the difficulties she faced while navigating Mount Everest, the one thought that kept her going — and how she wants to climb many more mountains now.




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Cos use foreign money for political funding. Isn’t that influencing polls?

A recent Intelligence Bureau (IB) report has claimed that some well-known NGOs are working to stall economic development at the behest of their foreign donors. Activists and rights groups have been up in arms ever since the report was leaked.




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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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Indian American Christians condemn assassination of Bhatti

Strongly condemning the assassination of Shahbaz Bhatti, the Federation of Indian Christians Organisations of North America appealed to Islamabad to bring the perpetrators of the "dastardly" crime to justice.




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Indian-American scientists develop alternative to radio tags

A team of Indian-American scientists has developed a smart tracking system, which could very well provide an honourable alternative to the radio tags.




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S African-Indian women get 3-yr jail for fraud

An Indian-origin woman and her mother were sentenced to three years in prison by a South African court, which found them guilty of arranging a fake certificate of marriage to inherit property of their landlord, who died of poisoning.




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Indian girl raped, murdered and stuffed inside suitcase in Australia

24-year-old Tosha Thakkar was last seen alive on March 9 in Sydney. Her alleged attacker, Daniel Stani-Reginald, has been denied bail.




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Indian dentists caught in UK red tape

Several dentists from India and other non-EU countries have been caught in bureaucratic wrangles between professional governing bodies in Britain, a leading migrants campaign group said today.




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Indian-origin Canadian gets life term for killing wife

A Canadian court has sentenced an Indian-origin man to life in prison for murdering his pregnant wife in 2006.




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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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Indian connection to prince William and Kate Middleton's wedding cake

Had it not been for the encouragement of her Gujarati husband Kishore Patel, Fiona Cairns may have never made the leap from graphic design to luxury baking.




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Coming to UP? You can use your own vehicle

More than 1.48 lakh people registered on the government's Jan Sunwai portal on Thursday, requesting to be brought back to UP from other states that they have been stuck in since the lockdown was imposed.




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Delhi Covid-19 cases mount to 6,318; toll 68

The total number of coronavirus cases in the national capital climbed to 6,318, with 338 new cases and two fresh deaths being reported on Friday, according to the Delhi government authorities.




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Plea on metro card-address proof linking declined




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Man who died of cardiorespiratory arrest tests +ve




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Motorola Edge, Motorola Edge+ launched: Here are the specifications, price, availability

Motorola is back in the flagship game with premium Edge series.




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USGS releases first comprehensive geological map of moon using Apollo data

The new map explains the 4.5-billion-year-old history of our neighbour in space.




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NASA's Hubble captures breakup of comet ATLAS into more than two dozen pieces

Hubble identified about 30 fragments on April 20, and 25 pieces on April 23.




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Astronomers discover closest black hole to earth, can be seen with naked eye

The finding was published in the journal Astronomy & Astrophysics.






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'Instagram has given my career a boost'

'I have started getting a lot of messages from people, directors, photographers...and I realised the importance of being visible.'





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'It's because of Bigg Boss that I am here'

'So many things opened up for me after I did the show.'




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'I can be a badass girl'

'If I look in a certain way, have an innocent face, I will only get offers for the girl-next-door roles. As an actor and creative person, you want to explore and experiment more but you don't get the opportunity. That gets frustrating at times.'




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'I can't imagine how A-list actors manage their lives'

'Sometimes, I wish someone would tell me that this will happen at this point in time, so I know how my life will be. I don't know what my evening is like. I don't know what my tomorrow will be like. The uncertainty sometimes takes a toll on me.'




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'People say the ghosts in my films were not scary'

'Films were made on a very low budget, so if there was a small defect, we would let it pass, and audiences often didn't catch those defects.' Shyam Ramsay tells us his 'horror' story.




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'I can't believe there are two Constitutions in India'

'India is called the largest democracy in the world, and one cannot believe that there are two Constitutions, two penal codes and two sets of laws.'





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'I cannot run away from TV roles'

'I am learning good things and trying to avoid the bad. I am moving ahead with a positive attitude. That is my biggest achievement.'