The Lab Notes

In December 2017 the United Nations proclaimed that 2019 will be international year of the Periodic Table of the Chemical Elements.[1] This coincides with the 150th anniversary of the periodic system discovered by Dmitry Mendeleev in 1869. We at Scientific Update love a good celebration so over the coming months, and in honour of this…

The direct halogenation of phenols using electrophilic halogenating reagents such as NBS are frequently used to prepare halogenated phenols. The problem with this method is that selectivity can often be low- the ortho- isomer is usually the minor component in a statistical mixture due to steric and electronic effects, and over reaction to give polyhalogenated…

A new paradigm in drug development began in the spring of last year with the Food and Drug Administration’s (FDA’s) approval of Teva pharmaceuticals’ VMAT2 inhibitor deutetrabenazine as a new chemical entity (NCE) under its 501(b)(2) legislation. This molecule is unique in that it is the first deuterium-substituted drug to reach the market and heralds…

The generation of lithium-alkoxide based aryl and heteroaryl Grignard reagents by Mg-Br/Cl exchange in toluene- increased reactivity and wide applicability. Organomagnesium-based organometallics are used extensively in organic chemistry.[1] Historically the reagents were prepared by direct insertion of magnesium metal into organic halides. With demand for more industrially applicable methods, halogen-magnesium exchange using alkyl magnesium halides…

A highly diastereoselective chloride-ion driven dynamic kinetic resolution of a phosphinate ester- a key step in the synthesis of Fosdevirine Fosdevirine (or GSK2248761A, top figure) is a non-nucleoside reverse transcriptase inhibitor, originally discovered by Idenix pharmaceuticals for the treatment of HIV infection. The structure is somewhat unusual in that it contains a phosphorus stereogenic centre-…

One might think that this hard-hitting, students best friend (it will reduce just about anything given the right conditions and is the go-to reducing agent for exam questions involving a reduction) has little more to offer to the practising chemist. However, a recent paper by Harder etal (Angew Chem Int Ed. 2018, 57(24), 7156) demonstrates…

  A patent issued this month cites the use of catalytic tetrabutylammonium bromide (TBAB) in the ring opening esterification of glycidyl ethers using acrylic acid and methacrylic acid (see Example 7). In PTC esterifications, we typically expect the presence of a base to form the carboxylate salt from the acid then the quat acrylate would…

I am delighted to share with you the announcement of a new award and a 'call for nominations'. The '1st Dr Margaret Faul Women in Chemistry Award' is intended to recognize and highlight outstanding contributions by young women to research in organic chemistry. The prize provided by Thieme includes an award of € 5,000. For more…

Britest is a leading exponent of whole process design for the chemical, pharma and other process manufacturing industries. We are pleased to be collaborating with Britest on our course 'Chemical Engineering: What Scientists and other Engineers Need to Know'. This course has been developed, and is presented, by chemical engineers and chemists who specialise in facilitating knowledge…

Scientific Update is delighted to announce the appointment of Dr John Studley, formerly Head of Process Chemistry for Vertex Pharmaceuticals, UK. John will join the team at Scientific Update in August 2018 as Scientific Director bringing over 20 years’ experience in drug discovery, process chemistry and scale up, having previously worked for Rhone-Poulenc, Oxford Asymmetry and Vertex…