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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


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


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


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


Louis Diorazio and co-workers at AstraZeneca recently published an article entitled “Toward a More Holistic Framework for Solvent Selection”, which describes the development of a solvent selection tool. Most solvent guides concentrate on Health and Environmental aspects of solvents, but where this new solvent selection tool differs is that it takes in to account issues


At the recent ‘Scale Up of Chemical Processes Conference’ in Baveno, Italy, John Snoonian of Sunovion discussed the development and scale up of a manufacturing route to make a 5HT4 partial agonist containing a 1,2,4-oxadiazole ring. During route scouting studies on the synthesis of the benzopyrazole an interesting solvent effect was observed – see Scheme


At the recent ‘Scale Up of Chemical Processes Conference’ in Baveno, Italy, Charles Papageorgiu of Eisai described the optimization of a borylation process to prepare boronic acid ML-826 (see Scheme 1). Scheme 1: Preparation of boronic acid ML-826 The original method using B2Pin2 and Pd(PPh3)2Cl2 as catalyst was extremely inefficient (9.25 day batch cycle time!)