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

In full flow-continuously battling bacteria with boron

Increasing multidrug resistance to antimicrobial agents, particularly in Gram-negative bacteria, is a significant global healthcare challenge. Carbapenem-resistant enterobacteriaceae (CRE) has been declared as one of the most urgent drug-resistant threats in the United States. Much like the cephalosporin B-lactams in the 1980’s, heavy clinical reliance on carbapenem b-lactam antibiotics over the past few decades has

Breaking up is hard to do

As synthetic chemists we are very familiar with making chemical bonds, particularly C-C bonds, and building complex molecules. Having said that, fundamentally, with sufficient energy and entropy in the driving seat, it should be quicker and easier to break molecules apart. Deconstructive processes are not, however, as common as one might think- particularly cleavage of

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,

Favipiravir and the battle against COVID-19

Whilst I was working towards my PhD in the early 90’s I remember reading ‘The Hot Zone’ by Richard Preston.1 Although non-fiction it read very much like a Michael Critchton2 thriller- describing the emergence and spread of viral hemorrhagic fevers and filoviruses such as Ebola and Marburg. Viruses such as Ebola are somewhat self-limiting in that the

Engineering life into new chemical transformations

Nature has had many generations to optimise its catalytic processes. As a result they are both extremely efficient and exquisitely selective. Biocatalysis is now very much a mainstay of industrial organic synthesis, particularly with the advent of protein engineering and directed evolution enabling the preparation of robust enzymes fine-tuned to a particular substrate. The importance

Syn-3-Fluoro-4-aminopiperidine- a story from multiple orientations

If Nature could re-write her proteinogenic amino acid instruction manual I’m fairly sure that a piperidine ring would feature in there somewhere. Perhaps in the spirit of less is more the pyrrolidine ring won out. Not so for human synthetic engineers- the piperidine ring is ubiquitous in pharmaceuticals, agrochemicals and advanced materials and is the

Hear Dr Will Watson’s Interview on CKHTV

Interview with Technical Director Dr Will Watson from Scientific Update on CKHTV Chemicals Knowledge Hub TV

The sun never sets on synthetic methodology- redox neutral organocatalytic Mitsunobu reactions

One of the things I enjoy most about science, and chemistry in particular, is that even processes that are well understood and used routinely, almost without thinking about them, can be re-invented. The allure of discovering new reactions and being at the forefront of a completely new area of research attracts many academics and students,

Alright with Rongalite! – Reagent of the Month

Sodium formaldehydesulfoxylate,1 first reported in the chemical literature in 1905 and marketed as Rongalite (Figure 1, CAS: 149-44-0, dihydrate: 6035-47-8, from the French word rongeage for decolorize)- is a commodity chemical used in the textile and dye industry as a bleaching agent and as a reducing agent in redox initiator systems for polymer formation. Historically it has

Enabling Synthesis in Fragment Based Drug Design (FBDD) with Emerging Technologies

Dr John Studley, Science Director at Scientific Update and Dr Rachel Grainger from Astex Pharmaceuticals got together ahead of our forthcoming Organic Process R&D Conference in Lisbon, Portugal on 23-25 September. Q: Dr John Studley (JS) Can you give us an overview of Fragment Based Drug Discovery (FBDD) and how you see the technique evolving over the next decade? A:

Scientific Update – changing with the times during covid-19

As businesses around the world have had to postpone and cancel live meetings, conferences and training courses in response to COVID-19 disease, workplace and group training has become one of the earliest and hardest-hit business activities. We have found that 100% of companies we work with across the globe, have had to postpone or cancel their