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Reactive extrusion (REX): the future of drug synthesis, continuous and solvent-free, is now!

The pharmaceutical industry is a major consumer of organic solvents, which are often dangerous, toxic and polluting, for the production of active pharmaceutical ingredients (APIs). To counter the ecological and economic challenges linked to the use of solvents in the fine chemicals industry, the Green Chemistry and Enabling Technologies team at IBMM has been involved for some time in developing mechanochemistry methods, mainly by ball-milling in the absence of solvent. However, milling is a batch process in a closed reactor and the scaling up of the corresponding reaction remains complicated. A radically different approach consisted in transposing these transformations into a continuous mode by using an extruder, a classical apparatus in the fields of polymer and food sciences, and which allows to cope with solids or very concentrated mixtures. The Green Chemistry and Enabling Technologies team, with the financial support of, among others, the Carnot Institute Chimie Balard Cirimat, was thus able to show that the reactive extrusion approach can easily create amide bonds present in 25% of the drugs on the market. This method was applied to the synthesis of two important APIs, teriflunomide (a treatment for multiple sclerosis) and moclobemide (an antidepressant). Thus, in 2 minutes, 11 grams of moclobemide were continuously synthesized, and just by feeding further the apparatus with starting material, the desired quantity could be prepared. One can already imagine the impact that these results will have in the pharmaceutical industry!

Amidation by reactive extrusion for the synthesis of active pharmaceutical ingredients teriflunomide and moclobemide

Matthieu Lavayssiere et Frédéric Lamaty, Chem. Commun. 2023 : lien.

Best award in the Mechanochemistry Challenge

The Green Chemistry and Enabling Technologies (F11) team was awarded the first prize in the Mechanochemistry Challenge (video competition) organized by Deasyl Innovation Green Chemistry in collaboration with the WAB group.

Organized during the summer of 2022, this competition aimed to show, in video, how mechanochemistry could make chemistry more environmentally friendly. With the involvement of all team members (interns, PhD students and permanent staff), this is now done for the Montpellier team.

The award ceremony took place in Frankfurt during Achema 2022 (August 22-26), during which Frédéric Lamaty gave a presentation on the importance of green chemistry in today’s and tomorrow’s challenges.

For more information, the video is available on the homepage of this website: www.greenchem.cnrs.fr

French-Polish symposium on serotonin type 6 receptor antagonists

French-Polish symposium on serotonin type 6 receptor antagonists

Neurodegenerative diseases have become the scourge of the 21st century, due to the lack of treatment and understanding of these diseases.

In this context, a symposium dedicated to recent advances in drug development for the treatment of diseases involving 5-HT6 receptors will take place on June 14-15, 2022 at the Scientific Center of the Polish Academy of Sciences in Paris.

Co-organized by the Scientific Center of the Polish Academy of Sciences in Paris, the Jagiellonian University-Collegium Medicum (Prof. Pawel Zajdel), the University of Montpellier, the Max Mousseron Institute of Biomolecules (Dr. Frédéric Lamaty) and the Montpellier Institute of Functional Genomics (Dr. Philippe Marin), it will provide an opportunity to discuss and exchange ideas on the role of 5-HT6 receptors in the treatment of diseases. It will provide an opportunity to discuss presentations ranging from the eco-compatible synthesis of biologically active compounds (flow chemistry, mechanochemistry), to the rational design of new potentially active molecules, through the identification of new potential biological targets.

Link:  https://paris.pan.pl/fr/events/antagonistes-des-recepteurs-de-la-serotonine-de-type-6-progres-recents-en-methodes-de-synthese-eco-compatibles-et-nouvelles-applications-therapeutiques/

 

The Legacy of Ei-ichi Negishi: Eternal Optimism & Excellence

This is the title of the article, published in the journal Chem, paying tribute to Prof. E. Negishi, 2010 Nobel Prize in Chemistry (together with Prof. A. Suzuki and R. F. Heck) for pallado-catalyzed cross-coupling reaction, who died June 6, 2021 at the age of 85. The co-authors, including Frédéric Lamaty, Research Director at CNRS and head of the Green Chemistry and Enabling Technologies team at IBMM, have left France at some point, some of them temporarily, to continue their doctoral or post-doctoral training at Purdue University (West Lafayette Indiana, USA) in the laboratory of the future Nobel Prize awardee. The article summarizes the major scientific contributions of Ei-chi Negishi, while including some impressions and anecdotes from daily-life in the laboratory. In September 2007, IBMM hosted Professor Ei-chi Negishi who presented at the University of Montpellier, as part of the seminars of the Doctoral School of Chemical Sciences, his research work concerning the zirconium-catalyzed asymmetric carbo-alumination reaction
(ZACA reaction).
 

Link to the article

Pawel Zajdel receives the French-Polish Binational 2021 Prize from the French Chemical Society

Pawel Zajdel, Professor of Medicinal Chemistry at the Medical College of Jagiellonian University (Krakow, Poland) and head of the Organic Chemistry department of the same university was awarded the prestigious French-Polish Binational 2021 Prize from the French Chemical Society. This award is a recognition of his scientific excellence and his commitment to numerous cooperation activities in France and in Montpellier. His research activity consists in developing ligands of proteins of interest such as G-protein coupled receptors (GPCRs), in particular serotonin and dopamine receptor modulators, for the treatment of neurodegenerative diseases of the central nervous system (Schizophrenia, Alzheimer’s disease).
 
His connection with France is very strong because he completed his thesis in 2006 under the supervision of the Profs. M. Pawłowski and J. Martinez. He was able to pursue this cooperation including, among other things, the supervision of two doctoral theses jointly supervised between the Jagiellonian University of Krakow in Poland and the University of Montpellier in France. This fruitful collaboration with Prof. J. Martinez, G. Subra and Dr. F. Lamaty and X. Bantreil from IBMM (Team Peptide and team Green Chemistry and Enabling Technologies) led to 21 joint publications, 3 patents and 5 common patent filings.
 

SCF Website

Xavier Bantreil, associate professor at the IBMM, was nominated as Junior member at the Institut Universitaire de France

Recruted at the Université de Montpellier in 2011 in the Green Chemistry and Enabling Technologies research team, supervised by Frédéric Lamaty, Xavier Bantreil was nominated as a Junior member of the IUF (Institut Universitaire de France) for a period of 5 years.

This appointment is recognition of the career path achieved and of the involvement, both in teaching (carried out at the Chemistry department of Sète of the IUT of Montpellier-Sète) and in research. It is also the result of working in an intellectual environment conducive to scientific exchanges and quality collaborations.

The 5-year delegation to the IUF should serve as a springboard for the development of new high-level research results. Green chemistry therefore has at least 5 good years ahead in Montpellier.

The list of laureates

CNRS Workshop Mechanochemistry for Companies

On July 5 and 6, 2021, the Green Chemistry and Enabling Technologies research team offers companies a training entitled “Mechanochemistry for eco-compatible synthetic chemistry”. The 2 days of training will be divided between lectures (but in a restricted committee) and practical sessions. This workshop is an exceptional opportunity to discover and practice mechanochemistry by taking advantage of the team’s expertise and equipment (vibratory ball-mill, planetary ball-mill, extruder).

Find the full description of the training on the CNRS Formation Entreprises website (link). There’s still time to sign up !