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Iron Catalysis in Organic Synthesis – A Critical Assessment of What it Takes To Make This Base Metal a Multitasking Champion

Industrial homogeneous catalytic processes are dominated by the use of expensive precious metals and rely on very efficient catalytic cycles for their cost effectiveness. Many of the processes carried out with precious metals are also achieved by iron catalysis, but often other processes compete and these chemistries have not been so widely used in industry,

To Telescope or Not to Telescope

Meanwhile in another presentation from the 4th Winter Process Conference this time from Alexandra Parker of AstraZeneca discussed the development of the manufacturing route to make Lesinurad (Zurampic) a selective uric acid reabsorption inhibitor approved for treatment of hyperuricemia associated with gout in combination with a xanthine oxidase inhibitor (XOI) in patients unable to achieve

Tautomeric Polymers

We are always taught that molecules which can exist in a number of existing tautomeric forms may be prone to polymorph formation as a result, but I came across a real example at our recent Winter Process Conference held at the University of Strathclyde in Glasgow in a presentation from Ivan Marziano of Pfizer. The

Alkyne to Alkene Reduction

The Lindlar reduction of alkynes to alkenes is well known but does not always work as well as we would like, so any new method for carrying out this potentially useful reduction is always of interest. Grela and a co-worker found that Hoveyda-Grubbs HG metathesis catalysts in the presence of NaH (20 mol %) and

Improving the Substrate Scope of the Kumada-Corriu Cross Coupling Reaction

The Ni or Pd catalysed Kumada-Corriu reaction between an aryl halide and a Grignard reagent is one of the original cross coupling reactions, and we all know that the Grignard reagent can react with suitable functional groups, such as carbonyls, on the aryl halide which limits it’s applicability.  Buchwald1 and Knochel2 have shown that by

Regioselective Chlorination of Phenols

Normally when one chlorinates a phenol one would expect to see perhaps 8:1 to 10:1 regioselectivity in favour of the para-isomer, but in this paper using N-chlorosuccinimide as the chlorinating agent, using the correct thiourea catalyst can give up to much better regioselectivity for either the o-chloro or p-chloro isomer depending on the thiourea catalysts

What does NDA Stand for?

Those of you in the pharma industry will be familiar with the acronym NDA standing for New Drug Application, but there could be a new chemical use for NDA as the sodium equivalent of LDA (lithium diisopropylamide), although the authors use NaDA, so perhaps we should use LiDA instead of LDA.  In this paper David

JUST FOR FUN…

What does 2 + 2 make? The mathematician will say 4 The chemist will say between 3.95 and 4.05 The lawyer will want to know what their fee will be for providing the information The accountant will say the answer is 4, but I’m sure you can manage with 1.6 The engineer will say the

UPDATED SOLVENT GUIDE AND SOLVENT NMR DATA

GSK were one of the first companies to publish a solvent selection guide and they have updated this gradually over the years, with the latest version of their guide being published just recently in Green Chemistry1. The new guide contains 44 more solvents taking the total number of solvents covered to 154. In addition, the

SOLVENT MAPPING

Another paper on the theme of solvents, is from Paul Murray working with the University College London and concerns the use of solvent maps and design of experiments (DoE). IN DoE solvent is usually considered to be a discrete or categorical variable, but by applying principle components analysis one can generate solvent maps so that solvent

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