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Synthesis of biaryls without using heavy metals- the photosplicing approach

Medicinal chemists love introducing aromatic rings into their pharmacophores. These flat rings make important lipophilic and pi-stacking interactions with proteins and are good synthetic handles for attaching functionality to reach and bind to all the nooks and crannies of an active site. With the advent of cross-coupling chemistry and the simplicity and efficiency of transition

Doing it Periodically-On The Table

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

Syntactic fantastic: A practical, ortho- selective mono-halogenation and phenylselenation of phenols by direct C-H halogenation.

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 Kinetic Kick-Start: Deutetrabenazine (AustedoTM)- the First FDA Approved Deuterated Drug

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

Oiling the cogs- Practical tips, useful facts and resources: Organometallic highlight:

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

Syntactic fantastic:

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-

Reagent of the month: Lithium Aluminium hydride

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

PTC – Tip of the Month – August 2018

  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

New Award for Women in Chemistry

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

Working with Britest on a new course on Chemical Engineering

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