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Wednesday 31 July 2013

The Sulfonamide Motif as a Synthetic Tool




Sulfonamides are well known motifs in medicinal chemistry, forming a large family of antibacterial agents as well as being found in numerous other drugs.  The chemistry of this functional group, however, is less well documented.  This review seeks to bring together the various applications and advantages of this motif in organic synthesis, which includes the sulfonamide as an activating group, protecting group, leaving group and as a molecular scaffold.
http://www.ingentaconnect.com/content/stl/jcr/2010/00000034/00000010/art00001


 The Sulfonamide Motif as a Synthetic Tool
Jonathan Wilden obtained his PhD from the University of Southampton in 2001 having worked on the total synthesis of the marine natural product pseudopterosin with Professor David Harrowven.  He then moved to the University of Sussex, Brighton, UK where his interest in sulfonamide chemistry began, working with Professor Steve Caddick.  In 2004 he was appointed lecturer at University College London where his research interests include the synthesis of medicinally important compounds and exploitation of the sulfonamide group in organic synthesis.

Tuesday 30 July 2013

Boron vapour trail leads to heterofullerenes

borafullerene
The simple route to borafullerenes could open up an interesting new avenue of heterofullerene research © Wiley-VCH
A team of scientists has developed a simple way to synthesise heterofullerenes – fullerenes with atoms other than carbon in their structure – by exposing fullerenes to boron vapour during their growth. They found that atom exchange with a carbon takes place to form a derivative known as borafullerene. The team believes the process can be easily scaled up and applied to other all-carbon analogues including nanotubes or graphene.
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Monday 29 July 2013

Nickel-Catalyzed Suzuki–Miyaura Couplings in Green Solvents

Figure

Nickel-Catalyzed Suzuki–Miyaura Couplings in Green Solvents

Publication Date (Web): July 23, 2013 (Letter)
DOI: 10.1021/ol401727y

The nickel-catalyzed Suzuki–Miyaura coupling of aryl halides and phenol-derived substrates with aryl boronic acids using green solvents, such as 2-Me-THF and tert-amyl alcohol, is reported. This methodology employs the commercially available and air-stable precatalyst, NiCl2(PCy3)2, and gives biaryl products in synthetically useful to excellent yields. Using this protocol, bis(heterocyclic) frameworks can be assembled efficiently.

Friday 26 July 2013

One-Pot Approach to α,β-Unsaturated Carboxylic Acids

thumbnail image: One-Pot Approach to α,β-Unsaturated Carboxylic Acids

 

One-Pot Approach to α,β-Unsaturated Carboxylic Acids

Carboxylation of alkynes with carbon dioxide in a one-pot approach could become a practical route to unsaturated carboxylic acids
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Concise Total Synthesis of a Newly Discovered Alkaloid

 








A concise synthesis of a novel alkaloid natural product with the pyrroloindoloquinazoline skeleton has been devised
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Tuesday 23 July 2013

Nano-Technoloogy Makes Medicine Greener


The ultra small nanoreactors have walls made of lipids. During their fusion events volumes of one billionth of a billionth of a liter were transferred between nanoreactors allowing their cargos to mix and react chemically. We typically carried out a million of individual chemical reactions per cm2 in not more than a few minutes. (Credit: Image courtesy of University of Copenhagen)http://www.sciencedaily.com/releases/2011/11/111103132357.htm
 Researchers at the University of Copenhagen are behind the development of a new method that will make it possible to develop drugs faster and greener. Their work promises cheaper medicine for consumers.
Over the last 5 years the Bionano Group at the Nano-Science Center and the Department of Neuroscience and Pharmacology at the University of Copenhagen has been working hard to characterise and test how molecules react, combine together and form larger molecules, which can be used in the development of new medicine.http://www.sciencedaily.com/releases/2011/11/111103132357.htm