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A Scalable Birch Reduction

The Birch reduction is a great reaction on small scale and can be carried out on large scale but requires specialist equipment to handle liquid ammonia (bpt -33°C) and it takes a significant amount of time to evaporate the ammonia at the end of the reaction. There have been various reports of alternative methods using

Biocatalysis: Enzymatic Synthesis for Industrial Applications

Biocatalysis is becoming ever more popular and prevalent in the synthesis of fine chemicals, agrochemicals and pharmaceuticals and is c becoming much more widely used in industrial chemical processes generally, so this review is very timely. The review includes sections on the synthesis of “Alcohols”, “Amines”, “Carbonyls, Carboxylic acids and Derivatives”, “Glycosylation”, “Complex Molecules” and

Iridium catalysed C-H borylation of alkyl C-H bonds

Two recent papers in Science have described Iridium catalysed C-H borylation of alkyl C-H bonds. The first paper1 reports a C-H borylation of primary C-H bonds.  Initial experiments showed that dibutyl ether (used as substrate and solvent) could be converted to BuO(CH2)4Bpin and similarly THF could be borylated in the 3-position with 2-methylphenanthroline (2-mphen) as

Designing Crystallisation Processes

Three recent papers from the groups of Nagy and Qu have discussed different options for designing and scaling up crystallisation processes to achieve polymorph control and obtain the correct particle size distribution (PSD). The first two papers1,2 describe using PAT (online analysis) with feedback control to design an antisolvent crystallisation process for indomethacin.  Each paper

A couple of interesting papers from Angewandte Chemie

1. Using an approved drug as a diazomethane surrogate1 A recent paper published in Angewandte Chemie describes the use of Temozolomide (TMZ) as a solid weighable diazomethane surrogate. TMZ is an approved drug and is the standout treatment for gliobastoma.  It is stable weighable solid, with reasonable water solubility.  Under physiological conditions , pH 7.4,

2 more cocrystal APIs on the market

Following a communication from a chemist at Merck / MSD I can now tell you about 2 more cocrystal APIs on the market – Lexapro (escitalopram oxalate) and Steglatro (ertugliflozin pyroglutamic acid cocrystal.  Lexapro is actually a cocrystal of the salt escitalopram oxalate with oxalic acid, similar in some ways to the Praziquantel intermediate naproxen

“Inconvenient Truths about Solid Form Landscapes”

The keynote speaker at our recent ‘Polymorphism and Crystallisation’ Conference in Boston was Dr Susan M. Reutzel-Edens from Eli Lilly, whose name will very familiar to anyone working in the solid form / crystallisation and she gave what one delegate described as “the best talk I have ever heard”. Now I can’t entirely agree with

3 cocrystal API’s now on the market

There are now 3 cocrystal API’s (Entresto, Suglat, and Depakote) on the market meaning that this area is no longer just an academic curiosity. Entresto is a cocrystal formed from the sodium salts of sacubitril and valsartan, but I do not know whether that is affected by the current furore over N-nitrosoamine impurities found in

Photo-Redox Catalysis

If you had suggested 10 years ago that it would be a good idea to try and develop some of the reactions that you can now carry out using photoredox catalysis, you would probably have been labelled as deluded, if you were not locked away for your own safety.  But photoredox catalysis has come a

Fluoride Sources for Halex Reactions

The halex reaction is a great way to introduce a fluorine atom in to an aromatic ring, but the reaction often requires high temperatures and or long reaction times if metal fluorides are used.  Tetralkylammonium fluorides are a better option due to their higher solubility in the reaction medium, however these salts are often hydrated

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