08 May 2012

Polymorph detection and quantification – a novel method

A novel method of detecting very low levels of different polymorphs using high-resolution X-ray powder diffraction with a synchrotron light source has been developed by Zach-Zambon Chemicals of Italy. Key to the project has been development of software to enable appropriate data presentation.

25 April 2012

ChemSpec Pharma Europe

13 - 14 June 2012

Gran Via Exhibition Center - Barcelona

Why not join us for any of three FREE to attend workshops during Chemspec Europe and which will be presented by Dr John Knight of Scientific Update LLP.

More information here>

23 April 2012

Peroxide-Mediated Wacker Oxidations

The Wacker oxidation is a powerful synthetic transformation for converting a terminal olefin into a ketone.

16 April 2012

Reductive Cleavage of Thioethers

Thiourea is often the reagent of choice for synthesising pyrimidines.  If a sulphur free pyrimidine is required the sulphur needs to be removed oxidatively or reductively.

09 April 2012

Transamidation of Primary Amides

Many primary amides are commercially available but the list of commercially available secondary amides is much smaller.

02 April 2012

Lean Filtration

Most products in the fine chemical and pharmaceutical industry are solids and are isolated by filtration or centrifugation. Many chemists and engineers have problems in filtration during early scale up, usually because of poor particle size distribution or presence of fines.

26 March 2012

Organofluorine Chemistry

The group of David O’Hagan at the University of St Andrews in Scotland has published a very useful review on Deoxyfluorination Reagents for Organic Synthesis [Al-Maharik N et al, Aldrichimica Acta, 2011, 44 (3) 65-75].

19 March 2012

Use of In Situ Raman, FBRM and ATR-FTIR Probes to Monitor a Solvent Mediated Polymorph Conversion

Scientists at the Universities of Brussels and Louvain in collaboration with UCB Pharma in Belgium have studied the solvent-mediated transformation of one polymorphic form of etiracetam ( the racemic intermediate in the synthesis of levetiracetam, marketed as Keppra by UCB Pharma) to the favoured form I prior to isolation of this desired form from methanol.  (OPRD, 2012, 16, 49-56).

05 March 2012

Amphoteric α-boryl aldehydes

Andrei Yudin and Zhi He reported in JACS 2011,133 (35), 13770 a new class of stable compound which shows some interesting reactivity.

27 February 2012

Additional Application of SMB

Amongst many great presentations at our recent conference in India I was particularly interested in and impressed by a presentation by Ganesh Pai of Arch Pharmalabs Ltd.

20 February 2012

Decarboxylative Strecker Reaction

A new twist on the traditional Strecker reaction has recently been published where you react a secondary amine such as proline with benzaldehyde and TMS cyanide in n-butanol as solvent at 200ºC to produce a 1-alkyl-2-cyanopyrrolidine.

13 February 2012

Carbon dioxide triggered copper catalysed furanone synthesis

During my general literature reading I have noted a continued growth in papers describing either entrapment of carbon dioxide or chemical transformations of the one-carbon unit.

13 February 2012

Palladium catalysed stereoselective [2,3]-rearrangements

Tambar et al (Syn Lett, 2011, (13) 1789) report on the use of chiral phosphoramidite ligand in conjunction with palladium acetate to promote the stereoselective rearrangement of N-oxides.

13 February 2012

Multi-component reactions involving arynes

I’ve been interested for some years now in multi-component reactions, noting a rise in the rate of publications as they are employed for accessing molecular diversity around a core skeleton as well as new reactions being designed.

13 February 2012

Selective reductive cyclisation to form quinolines

I have previously commented on the use of Hantzsch esters for carrying out reductions and so this paper caught my eye.