Archive for September, 2012

An alternative one-pot gold-catalyzed approach to the assembly of 11H-indolo[3,2-c]quinolines

In this HOT paper Antonio Arcadi, Università degli Studi di L’Aquila, and colleagues present a newly developed one-pot gold-catalysed approach to the assembly of 11H-indolo[3,2-c]quinolines from readily available unprotected 2-[2-(2-aminophenyl)ethynyl]anilines and aldehydes.

Arcadi et al. use the clever idea of first using a fast regio-selective intramolecular reaction, followed by a slower intermolecular condensation and subsequent cyclisation and final hydrogen transfer nicely provides a fast, synthetically efficient and elegant access to indolo[3,2-c]quinolines. With its broad scope, mild conditions and high regioselectivity this could be a valuable alternative to protocols previously described in the literature.

Find out more by downloading this paper today. It’s free to access for 4 weeks so grab it whilst you can.

An alternative one-pot gold-catalyzed approach to the assembly of 11H-indolo[3,2-c]quinolines
Giorgio Abbiati, Antonio Arcadi, Marco Chiarini, Fabio Marinelli, Emanuela Pietropaolo and Elisabetta Rossi
DOI: 10.1039/C2OB26380G

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Steric effects on the catalytic activities of zinc(II) complexes in the cleavage of the RNA and DNA model phosphates

This manuscript from Zhong-Lin Lu and co-workers presents the preparation of a series of mononuclear and dinuclear zinc(II) complexes with ligands bearing different numbers of N-methyl groups, and includes a thorough kinetic study towards the hydrolytic cleavage of RNA and DNA model substrates.

The study focuses on the influence of steric effects on the catalytic efficiency and for the first time probes the effect of N-methylation of triazacyclododecane ligands. The N-methylation substantially reduces the co-operative behaviour between mononuclear zinc complexes and for the dinuclear complexes the activities are also substantially reduced but are still faster than the background reaction without the metal-complex.

Find out more by clicking below… download it now, it’s free for 4 weeks!

Steric effects on the catalytic activities of zinc(II) complexes containing [12]aneN3 ligating units in the cleavage of the RNA and DNA model phosphates
Yang Song, Ju Zan, Hao Yan, Zhong-Lin Lu and Ruibing Wang
DOI: 10.1039/C2OB25624J

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Chemical biology and medicinal: Potential agents to treat Alzheimer’s disease

Scientists in Germany have worked on optimising compounds that reduce the formation of amyloid β-peptides, which play a crucial role in the development and progression of Alzheimer’s disease. The team varied the membrane anchor, spacer and pharmacophore building blocks on BACE1 inhibitors to make tripartite structures (assembled by covalent coupling of BACE1 inhibitors with membrane anchors via suitable spacers).

Several BACE1 inhibitors have already been reported, but here, the team has shown that the cellular activity of small-molecule BACE1 inhibitors can be significantly increased by membrane targeting via a spacer with a raftophilic membrane anchor.

Optimisation of BACE1 Inhibition of Tripartite Structures by Modification of Membrane Anchor, Spacer and Pharmacophore – Development of Potential Agents for the Treatment of Alzheimer’s Disease
Hans-Joachim Knölker
DOI: 10.1039/C2OB26103K

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Physical organic chemistry: An article collection

Physical organic chemistry, the study of the underlying principles and rationale of organic reactions which looks at the interrelationships between the structure and reactivity of organic molecules, now encompasses a wider range of contexts than ever before.

Making use of tools such as chemical kinetics, quantum chemistry, thermochemistry, chemical equilibrium and computational chemistry, to name but a few, researchers are investigating topics such as:

•    Supramolecular interactions, aggregation and reactivity
•    The computation of transition states and mechanisms
•    Molecular recognition, reactions and catalysis in biology
•    Materials where molecular structure controls function
•    Structure activity correlations
•    Mechanisms in synthesis and catalysis

To highlight some of the cutting edge research that ChemComm, Chemical Science and Organic & Biomolecular Chemistry receive we have collected a selection of articles for you to enjoy. These will be free to access until 25th September!

Click here for the full list of free articles

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Using Chemistry to improve Agricultural Productivity

Chemistry for Tomorrow’s World 2012: Using Chemistry to Improve Agricultural Productivity

6 pm, 26 September 2012
Chemistry Centre, Burlington House, London

Join us at the RSC’s Chemistry Centre in London to hear about how synthetic organic chemistry can help to feed the world.

Azoxystrobin is the world’s leading agricultural fungicide. It is a fully synthetic compound, whose invention was inspired by the structure and activity of the naturally-occurring fungicide strobilurin A. Today it is used worldwide to control fungi growing on over 120 types of crop, improving plant health, raising quality and increasing yield. The success of the project highlights the crucial importance of chemistry in meeting grand challenges such as global food security and the broader applicability of skills such as natural product synthesis. Our keynote speaker Dr John Clough led the team of chemists at Syngenta that invented azoxystrobin. He will discuss the key role that synthetic organic chemistry played in creating an effective and safe fungicide.

This event will be held in the Chemistry Centre on 26 September at the RSC’s recently refurbished building in Burlington House, London. Doors will open at 17:30 for refreshments. The event will begin at 18:00 and will finish with a wine reception. Please follow the link here for information and to register for the event.

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