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What’s New in Process Chemistry – Issue 64 December 2018
 
 
Enjoy the gin but spare a little thought for the tonic….

Gin is rapidly becoming the nations favourite tipple. Its undergone a modern renaissance with familiar trade names such as Gordon’s, Plymouth and London and multiple artisan distilleries appearing country-wide. It’s even drawn synthetic organic chemists out of the lab and into the refineries. This week at our 5th Winter Process Chemistry Conference in Manchester UK


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A concise total synthesis of Quinine and analogues via C-H activation

                    The naturally occurring cinchona alkaloids, and Quinine in particular, have been of interest to synthetic chemistry practitioners for many years, due ostensibly to its antimalarial activity, particularly against resistant strains of the disease. The original synthesis, by Woodward and Doering in 1944 was heralded as


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Antibiotics, synthetic organic chemistry and the war against the microbes:

One of the first encounters I had with complex structures and challenging organic synthesis was a course I took on the synthesis of antibiotics as an undergraduate chemist at Bath university almost thirty years ago. These molecules and I had had a love hate relationship for much of my early childhood, having consumed what must


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Bio-Transforming: Stereodivergent cyclopropanation of non-activated alkenes  

One of the challenges associated with biocatalysis is the resulting stereochemistry is not always easy to predict and more often than not gives the unwanted isomer. The problem is compounded if the substrate has limited steric or electronic components to aid stereocontrol. A way around this problem is to engineer the wildtype protein. A resect


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Biocatalytic oxidation and synthesis of Esomeprazole

Esomeprazole is a proton pump inhibitor developed by Astra Zeneca in 2001 and marked under the trade name Nexium. Esomeprazole is the S-enantiomer of omeprazole (the racemate) and is an example of the controversial so-called “chiral switch” in with single isomers are developed and marked as having improved pharmacodynamic or phmacokinetic properties over the originally


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The Chichibabin amination reaction

         2-Aminopyrides are useful synthetic intermediates and pharmacophores in a number of drugs.[1] The Chichibabin reaction, developed in the 1900’s gives a direct method for the amination of pyridine and pyridine derivatives (azines and azoles) using sodium or potassium amides. Intramolecular amination reactions are also known. The reaction can be run either


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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


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Cyanomethylene trimethylphosphorane (CMMP)- a safer reagent for Mitsunobu couplings

The Mitsunobu reaction is a powerful coupling method for alkylation of various nucleophiles (H-A) with alcohols (R-OH).[1] The classical conditions use a redox system comprising of an azodicarboxylate (such as diethylaziodicarboxylate, DEAD) and a phosphine (normally triphenylphosphine, TPP). The alcohol is essentially activated in situ and coupling occurs with the generation of the phosphine oxide


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Protecting group free radical C-H trifluoromethylation of peptides  

The resurgence of peptide and protein-based therapeutics and the demand for chemical probes to elucidate complex biological pathways has driven the development of synthetic chemistry compatible with post translational modification and/or bioconjugation. The use of fluorine-modified biomolecules has enabled the 19F nucleus to be used in NMR experiments to study protein structure, dynamics and protein-ligand


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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


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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


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5th Winter Process Chemistry Conference & Exhibition
11 December 2018 -
13 December 2018

14th Winter Conference on Medicinal & Bioorganic Chemistry
27 January 2019 -
31 January 2019

Flow Chemistry and Continuous Processing Conference
08 April 2019 -
09 April 2019

Polymorphism and Crystallization Conference
08 April 2019 -
09 April 2019

Catalysis in the Fine Chemicals Industry
14 May 2019 -
15 May 2019

 
 
Practical Crystallization & Polymorphism
07 February 2019 -
08 February 2019

Chemical Development & Scale-Up in the Fine Chemical & Pharmaceutical Industries
11 February 2019 -
13 February 2019

Practical Crystallization & Polymorphism
28 February 2019 -
01 March 2019

Chemical Development & Scale-Up in the Fine Chemical & Pharmaceutical Industries
04 March 2019 -
06 March 2019

Organic Synthesis: A Toolkit for the Industrial Chemist
13 March 2019 -
15 March 2019

 
 
Temperature Control in the Process Environment
23 January 2019
Olefin Metathesis
27 March 2019
 
 
 
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