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Contemporary Synthetic Chemistry in Drug Discovery Themed Issue Launched

Organic and Biomolecular Chemistry (OBC) is delighted to announce a high-profile web themed issue on Contemporary Synthetic Chemistry in Drug Discovery. The guest editors for this issue are Professor Angela Russell (University of Oxford, UK), Professor Douglas E. Frantz (The University of Texas at San Antonio, USA), Dr Matthew Duncton (Rigel, San Francisco, USA), Dr Graham Wynne (University of Oxford, UK) and Dr Shane Krska (Merck, Boston, USA).

Deadline for Submission: 30 April 2016

If you are interested in taking part in this issue, please email OBC: obc-rsc@rsc.org

Manuscripts can be submitted using the Royal Society of Chemistry’s online article submission service. Please clearly state that the manuscript is submitted for the themed issue on Contemporary Synthetic Chemistry in Drug Discovery.

The level of quality of this issue will be high, and all manuscripts will undergo the journal’s normal peer review process. Guidelines are available at rsc.li/1K0EgYx and rsc.li/1OoQWQh



Scope of the issue

This issue aims to demonstrate the importance of synthetic chemistry in drug discovery. Specifically it will highlight how synthetic methods can be used to address hurdles currently being faced in modern medicinal chemistry. Areas falling within the scope of the issue include:

•    CH-Functionalization, including late-stage CH-functionalization & CH-functionalization via biomimetic catalysis
•    Fluorination chemistry, including late-stage fluorination, CF3, SCF3 & SF5 chemistry
•    Asymmetric chemistry, including use of organocatalytic methods
•    Synthesis of compounds with enhanced 3-dimensional character (including cross-coupling & other metal-catalyzed reactions, particularly in relation to sp3-functionalization)
•    Modern heterocyclic chemistry including synthesis of novel heterocycles, highly-decorated heterocycles & synthesis/use of small heterocyclic groups (e.g. oxetanes, azetidines, etc.)
•    Modern synthetic techniques, including flow chemistry, automated synthesis, high-throughput synthesis, microwave-assisted chemistry, multi-component reactions & sustainable chemistry
•    Synthesis/modification of natural products, or natural-product-like compounds (diversity-orientated synthesis)
•    Synthesis utilizing enzymatic chemistry and its use in drug discovery
•    The use of novel reagents/reactions in drug discovery


All submissions should clearly show/explain what challenge within drug discovery is being addressed by the presented work. Articles covering general organic synthesis without this connection are not suitable for this issue.

Inclusion of biological data is not a requirement for submission but you are welcome to include any such data that you feel supports your article. Please note that the main focus of the manuscript should be on the organic synthesis and not the medicinal chemistry.

To view recent articles or find out more about OBC, please visit the journal’s homepage:

Organic & Biomolecular ChemistryRapid publication of high quality organic chemistry research

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RSC Organic Division Poster Symposium 2015

RSC Organic Division Poster Symposium 2015, headline sponsored by F. Hoffmann-La Roche, Ltd.

Abstract submission is now open.

This poster symposium for final year organic chemistry PhD students will take place at The Royal Society of Chemistry at Burlington House, in London, Monday 30 November 2015.

The closing date for submissions is Wednesday 30 September 2015.
Get more information or submit an abstract now.


This symposium offers final year PhD students a chance to showcase their research to their peers, leading academics and industrial chemists. It is open to all branches of organic chemistry – in its broadest interpretation – and has a tradition of being the most competitive and highly-regarded organic chemistry symposium for PhD students in the UK and Ireland.

There will be a first prize of £500, two runner-up prizes of £250, and a ‘selected by Industry’ prize – also of £500. Industrial delegates will select this winner based on the potential for application in an industrial context.

We would like to thank F. Hoffmann-La Roche, Ltd. and our industry sponsors for their generous support of this event.

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Fast decisions and publication in Organic & Biomolecular Chemistry

At Organic & Biomolecular Chemistry we understand the importance of getting your work seen by your peers in the organic chemistry community as soon as possible.

This is why we get you a decision as fast as possible without compromising on the quality of the review process.

The average time for you to get the first decision on your Organic & Biomolecular Chemistry submission is just:

Communications: 12 days
Papers: 19 days

What is more, from submission to publication of the fully edited version of your manuscript (including time for author revisions) it takes on average:

Communications: 36 days
Papers: 49 days

This is based on all articles sent out to referees in the period January–June 2015. Articles that did not pass an initial assessment have not been included in this calculation.



Want to know more about OBC and the benefits of publishing your work with us?

Want to experience the same service as your colleagues that publish with us?

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Carbohydrate Active Enzymes in Medicine and Biotechnology Meeting

Carbohydrate Active Enzymes in Medicine and Biotechnology Meeting
19-21 August 2015, St Andrews, UK

Oral and poster abstract submission deadline is 26 June.

Register now to secure your place – members of the Royal Society of Chemistry are eligible for a reduced rate. The meeting will cover the following topics:

  • Insights into carbohydrate active enzymes in medicine
  • Use of carbohydrate active enzymes in biotechnology
  • Understanding mechanism and structure of carbohydrate active enzymes
  • Exploiting carbohydrate active enzymes in biosynthesis

The three day conference programme comprises of 15 plenary talks, including Prize and Award Lectures presented by Sabine Flitsch – Royal Society of Chemistry Interdisciplinary Prize 2014, Gideon Davies – Royal Society of Chemistry Khorana Prize 2014 and Glyn Hemsworth – Biochemical Society Early Career Research Award.

For more information and to book your place please visit our event page.

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Introducing OBC Associate Editor Prof. Christian Hackenberger

Professor Christian Hackenberger has joined Organic & Biomolecular Chemistry as an Associate Editor. We are delighted to welcome him to the team and look forward to working with him over the coming years.

Christian completed his graduate studies with Prof. Sam Gellman (Univeristy Wisconsin-Madison) and his doctoral work with Prof. Carsten Bolm at the Rhine-Westphalia Institute of Technology Aachen. After his postdoctoral stay in the group of Prof. Barbara Imperiali at MIT he started his own lab at the Freie Universität Berlin as a FCI-Liebig-Scholar and Emmy Noether Fellow in 2005. In 2012, he accepted a position as the Leibniz–Humboldt Professor for Chemical Biology to the Leibniz Institut for Molecular Pharmacology and the Humboldt Universität zu Berlin.

Christian’s research interests focus around studying the biology, function and pharmacological potency of naturally and unnaturally modified peptides and proteins and include:

  • Development of ligation and modification strategies for the synthesis of functional proteins
  • Bioorthogonal Staudinger phosphite and phosphonite reactions
  • Labeling strategies for antibody ‐ and nanobody conjugates
  • Intracellular delivery and targeting
  • Protein and peptide PEGylation
  • Functional investigation of the Alzheimer‐relevant Tau protein
  • Engineering of protein‐based multivalent scaffolds
  • Metabolic oligosaccharide engineering

On starting his new role as Associate Editor for  Organic & Biomolecular Chemistry Christian said:

I am delighted to act as an associate editor to OBC. Without a question I am very happy about the nomination from the editorial board, especially because I published my very first independent paper back in 2006 in OBC. This new job is both a privilege and an honor to serve the community and work with the editorial team of the Royal Society of Chemistry

Submit a manuscript for Christian to handle
Visit Christian’s homepage

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Organic chemistry’s complexity conundrum

Organic synthesis is often heralded as more art than science. An organic chemist’s eye for complexity, breaking down structures into simpler forms, is honed and nurtured over decades. But, is it possible to take this seemingly intangible skill and quantify it, putting a simple number on how complex a chemical structure actually is?

Process chemists Martin Eastgate and Jun Li, at Bristol-Myers Squibb (B-MS) in the US have developed a tool to do just that, generating a unique index they have termed a molecule’s current complexity, which also accounts for changes over time due to the impact of new technologies.


Read the full Chemistry World story»

Read the original Organic & Biomolecular Chemistry article – it’s free to access until 2nd July:
Current complexity: a tool for assessing the complexity of organic molecules

Jun Lia and Martin D. Eastgate
Org. Biomol. Chem., 2015, DOI: 10.1039/C5OB00709G

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Agri Innovation 2015

Join us on 22 April at the Society of Chemical Industry in London for Agri Innovation 2015: Emerging Technologies in Crop Research

This one-day meeting aims to provide an update on several areas of crop research, including identifying target proteins for crop protection ingredients, the synthesis of new crop protection agents and understanding the mechanisms of resistance and immunity in plants and insects. If you are working in organic synthesis, chemical biology or biochemistry in relation to crop science, this meeting will provide an opportunity to catch up on the latest developments. Speakers from academia and industry from across Europe will come together to present and discuss the latest developments in this area.

The meeting is jointly run by the Royal Society of Chemistry, the Society of Chemical Industry Agrisciences Group and AGRI-net, the agriscience chemical biology network. For more details and to register, please visit the website.

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New Editorial Board Chair

Prof. Andrei YudinWe are delighted to announce that Professor Andrei Yudin has become the Chair of the Editorial Board for Organic & Biomolecular Chemistry.

For the past 3 years Andrei has been handling manuscripts for OBC as an Associate Editor, but with his move to his new role he will no longer be handling manuscripts himself.

The previous Chair, Professor Jeff Bode, passed over the reins to Andrei at the begining of 2015, and this brings his time on the OBC Editorial Board to a close. Professor Paolo Scrimin‘s time on the Editorial Board has also drew to a close at the end of 2014. We would all like to thank both Jeff and Paolo for the many years of service and the invaluable contributions they have made in helping to guide the journal.

About Andrei:

Professor Andrei Yudin obtained his B.Sc. degree at Moscow State University and his Ph.D. degree at the University of Southern California under the direction of Professors G. K. Surya Prakash and George A. Olah. He subsequently took up a postdoctoral position in the laboratory of Professor K. Barry Sharpless at the Scripps Research Institute. In 1998, he started his independent career at the University of Toronto. He received early tenure, becoming an Associate Professor in 2002, and received an early promotion to the rank of a Full Professor in 2007.

Amongst Professor Yudin’s awards are the CSC Award in Combinatorial Chemistry, the 2004 Amgen New Faculty Award, the 2010 CSC Merck-Frosst Therapeutic Center Award, the 2010 Rutherford Medal of the Royal Society of Canada, the 2011 University of Toronto Inventor of the Year Award, and the 2015 Bernard Belleau Award in Medicinal Chemistry. Professor Yudin is a Fellow of the Royal Society of Canada.

Andrei’s Homepage: http://www.chem.utoronto.ca/wp/yudinlab/

Andrei also maintains a science blog – Amphoteros – that aims to illuminate the ongoing synthetic and chemical biology efforts in his lab and to discuss general advances in science, both from the past and present.

Below is his blog following our Editorial Board meeting at the end of last year.

Some news from London

Posted on November 20, 2014

Over the past several days I have been in London, England, where I attended the Fall Board Meeting of Organic and Biomolecular Chemistry. Richard Kelly, the Managing Editor of this RSC publication, has put this meeting together in the Mayfair district of London. Jeff Bode (ETH, Zurich) is stepping down as the Board Chairman and I will be taking over his responsibilities from January 2015. I have to tip my hat off to Jeff for his leadership over the past several years. I have thoroughly enjoyed my role of one of the Associate Editors. The difference now will be that I am no longer going to handle manuscripts, but will instead oversee some strategic areas for growth and improvement. I think this will be very exciting. Earlier this week, I had a lot of fun together with Jeff as well as Ashraf Brik of Ben Gurion University, Margaret Brimble of the University of Aukland, Tony Davis of the University of Bristol, Jonathan Clayden of the University of Manchester, Pauline Chiu of the University of Hong Kong, and Paolo Scrimin of the University of Padova. Unfortunately, Jin-Quan Yu of Scripps was not able to make it to this meeting. Along with Margaret and I, Jin-Quan is one of OBC’s Associate Editors.

In terms of chemistry, I actually wanted to share something that relates to the work of Margaret Brimble (she flew in all the way from New Zealand to meet us). Margaret brought along some exciting news: NNZ-2566, a molecule developed as part of a collaboration between her lab and Neuren Pharma, was recently approved by the FDA, which has granted orphan drug designation to NNZ-2566 for treatment of Fragile X Syndrome. This tripeptide also demonstrates neuroprotective efficacy in models of traumatic brain injury such as concussion. Evidently, the U.S. Army is very interested in NNZ-2566, although not much is known about the mechanism of action of this exciting compound. What I found remarkable is that the tripeptide is orally bioavailable. The C-methyl proline residue makes this molecule considerably more stable than the corresponding non-methylated congener. The methyl group really “messes up” with the nearby amide bond, which apparently drives the logD down and improves the pharmacological profile of NNZ-2566. I have always thought that there is something special about C-methylproline…

http://www.neurenpharma.com/irm/content/nnz-2566-in-rett-syndrome.aspx?RID=330

Make sure you don’t miss out on the latest journal news by registering your details to receive the regular Organic & Biomolecular Chemistry e-alert.

Follow us on Twitter @OrgBiomolChem

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Take 1…minute for chemistry in health

Can you explain the importance of chemistry to human health in just 1 minute? If you’re an early-career researcher who is up to the challenge, making a 1 minute video could win you £500.

The chemical sciences will be fundamental in helping us meet the healthcare challenges of the future, and we are committed to ensuring that they contribute to their full potential. As part of our work in this area, we are inviting undergraduate and PhD students, post-docs and those starting out their career in industry to produce an original video that demonstrates the importance of chemistry in health.

We are looking for imaginative ways of showcasing how chemistry helps us address healthcare challenges. Your video should be no longer than 1 minute, and you can use any approach you like.

The winner will receive a £500 cash prize, with a £250 prize for second place and £150 prize for third place up for grabs too.

Stuck for inspiration? Last year’s winning video is a good place to start. John Gleeson’s video was selected based on the effective use of language, dynamic style, creativity and its accurate content.

The closing date for entries to be submitted is 30 January 2015. Our judging panel will select the top five videos. We will then publish the shortlisted videos online and open the judging to the public to determine the winner and the runners up.

For more details on how to enter the competition and who is eligible, join us at the Take 1… page.

Good luck!

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HOT Organic & Biomolecular Chemistry articles

The following Organic & Biomolecular Chemistry articles have all been recommened by the reviewers of the articles as being particularly interesting or particularly significant research. These have all been made free to access until 30th November. The order they appear in the list holds no special meaning or ranking.

Design strategies for bioorthogonal smart probes
Peyton Shieh and Carolyn R. Bertozzi
DOI: 10.1039/C4OB01632G, Review Article

bioorthogonal smart probes


Stereoselective intermolecular [2 + 2]-photocycloaddition reactions of maleic anhydride: stereocontrolled and regiocontrolled access to 1,2,3-trifunctionalized cyclobutanes
Florian Hernvann, Gloria Rasore, Valérie Declerck and David J. Aitken
DOI: 10.1039/C4OB01383B, Paper

Stereoselective intermolecular [2 + 2]-photocycloaddition reactions of maleic anhydride


Towards novel efficient and stable nuclear import signals: synthesis and properties of trimethylguanosine cap analogs modified within the 5′,5′-triphosphate bridge
Malgorzata Zytek, Joanna Kowalska, Maciej Lukaszewicz, Blazej A. Wojtczak, Joanna Zuberek, Aleksandra Ferenc-Mrozek, Edward Darzynkiewicz, Anna Niedzwiecka and Jacek Jemielity
DOI: 10.1039/C4OB01579G, Paper

trimethylguanosine cap analogs


Catalytic asymmetric synthesis of the pentacyclic core of (−)-nakadomarin A via oxazolidine as an iminium cation equivalent
Nobuya Tsuji, Michael Stadler, Naoya Kazumi, Tsubasa Inokuma, Yusuke Kobayashi and Yoshiji Takemoto
DOI: 10.1039/C4OB01678E, Communication

atalytic asymmetric synthesis of the pentacyclic core of (−)-nakadomarin A


Short and efficient synthesis of fluorinated δ-lactams
Thomas J. Cogswell, Craig S. Donald, De-Liang Long and Rodolfo Marquez
DOI: 10.1039/C4OB01547A, Paper

synthesis of fluorinated δ-lactams


An efficient route to synthesize isatins by metal-free, iodine-catalyzed sequential C(sp3)–H oxidation and intramolecular C–N bond formation of 2′-aminoacetophenones
Venkatachalam Rajeshkumar, Selvaraj Chandrasekar and Govindasamy Sekar
DOI: 10.1039/C4OB01564A, Paper

 I2-catalyzed synthesis of isatins


5-Nitroindole oligonucleotides with alkynyl side chains: universal base pairing, triple bond hydration and properties of pyrene “click” adducts
Sachin A. Ingale, Peter Leonard, Haozhe Yang and Frank Seela
DOI: 10.1039/C4OB01478B, Paper

5-Nitroindole oligonucleotides with alkynyl side chains


Cross-strand histidine–aromatic interactions enhance acyl-transfer rates in beta-hairpin peptide catalysts
M. Matsumoto, S. J. Lee, M. R. Gagné and M. L. Waters
DOI: 10.1039/C4OB01754D, Paper

 Cross-strand histidine–aromatic interactions enhance acyl-transfer rates in beta-hairpin peptide catalysts


The asymmetric syntheses of pyrrolizidines, indolizidines and quinolizidines via two sequential tandem ring-closure/N-debenzylation processes
Stephen G. Davies, Ai M. Fletcher, Emma M. Foster, Ian T. T. Houlsby, Paul M. Roberts, Thomas M. Schofield and James E. Thomson
DOI: 10.1039/C4OB01737D, Paper

asymmetric syntheses of pyrrolizidines, indolizidines and quinolizidines


Organocatalytic Michael addition–lactonisation of carboxylic acids using α,β-unsaturated trichloromethyl ketones as α,β-unsaturated ester equivalents
Louis C. Morrill, Daniel G. Stark, James E. Taylor, Siobhan R. Smith, James A. Squires, Agathe C. A. D’Hollander, Carmen Simal, Peter Shapland, Timothy J. C. O’Riordan and Andrew D. Smith
DOI: 10.1039/C4OB01788A, Paper

Organocatalytic Michael addition–lactonisation of carboxylic acids

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