A Kinetic Kick-Start: Deutetrabenazine (AustedoTM)- the First FDA Approved Deuterated Drug
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| 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 Read More | |
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Oiling the cogs- Practical tips, useful facts and resources: Organometallic highlight:
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| 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 Read More | |
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Reagent of the month: Lithium Aluminium hydride
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| 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 Read More | |
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PTC – Tip of the Month – August 2018
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| 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 Read More | |
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Chromatographic Processes
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| Preparative chromatography is a versatile purification technique used in various industrial sectors including petrochemistry, sugar production, pharmaceutical and fine chemistry, to name only a few. While this technology is often considered complex, expensive and sometimes not scaleable, industrial success stories prove the opposite. In our recent webinar, Dr. Pfister from Ypso-Facto presented a reliable approach Read More | |
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Recent Progress in Decarboxylative Oxidative Cross Coupling
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| A short review article, also from the group of Igor Larrosa at Manchester, on the use of aromatic carboxylic acids as coupling partners in biaryl synthesis, appeared earlier in European Journal of Organic Chemistry (2017, 3517-3527). It is suggested in the micro-review that benzoic acid derivatives are atom-economic alternatives to traditional cross coupling partners, and Read More | |
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Transition-Metal-Free Decarboxylative Bromination of Aromatic Carboxylic Acids
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| The brominative decarboxylation reaction was demonstrated over a hundred and fifty years ago by Borodin (the famous composer, whose day job was as Professor of Organic Chemistry) and later developed by Hunsdiecker, whose name the reaction now bears. From an industrial viewpoint the transformation would be useful but the need to have a stoichiometric silver Read More | |
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Utilization of fluoroform for difluoromethylation in continuous flow: a concise synthesis of α-difluoromethyl-amino acids
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| Published in Green Chemistry in 2018 C. Oliver Kappe is our tutor on our Flow Chemistry course and this abstract was published in Green Chemistry showing a collaboration with Lonza in making an API in flow. Abstract: Fluoroform (CHF3) can be considered as an ideal reagent for difluoromethylation reactions. However, due to the low reactivity Read More | |
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| 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 Read More | |
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New Award for Women in Chemistry
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| 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 Read More | |
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