Amidation by reactive extrusion for the synthesis of active pharmaceutical ingredients teriflunomide and moclobemide DOI Creative Commons
Matthieu Lavayssiere, Frédéric Lamaty

Chemical Communications, Journal Year: 2023, Volume and Issue: 59(23), P. 3439 - 3442

Published: Jan. 1, 2023

The solventless synthesis of an amide was performed in a twin-screw extruder the presence coupling agent, providing high yielding and productive method. reaction conditions were optimized to prepare APIs, teriflunomide moclobemide.

Language: Английский

Sustainability Assessment of Mechanochemistry by Using the Twelve Principles of Green Chemistry DOI
Karen J. Ardila‐Fierro, José G. Hernández

ChemSusChem, Journal Year: 2021, Volume and Issue: 14(10), P. 2145 - 2162

Published: April 9, 2021

In recent years, mechanochemistry has been growing into a widely accepted alternative for chemical synthesis. addition to their efficiency and practicality, mechanochemical reactions are also recognized sustainability. The association between Green Chemistry often originates from the solvent-free nature of most protocols, which can reduce waste production. However, satisfies more than one Principles Chemistry. this Review we will present series examples that clearly illustrate how significantly contribute fulfillment in holistic manner.

Language: Английский

Citations

471

Liquid‐Assisted Grinding Mechanochemistry in the Synthesis of Pharmaceuticals DOI

Ping Ying,

Jingbo Yu, Weike Su

et al.

Advanced Synthesis & Catalysis, Journal Year: 2021, Volume and Issue: 363(5), P. 1246 - 1271

Published: Jan. 21, 2021

Abstract Mechanochemical reactions by milling, grinding or other types of mechanical action have emerged as a salient green approach because its wide applications towards academic and industrial chemical communities in sustainable solvent‐free/solvent‐less processes. Liquid‐assisted (LAG) an extension traditional solvent‐free mechanochemical techniques which small amount liquid is used additive to enhance and/or control reactivity, has been fruitfully applied the screening inclusion compounds, cocrystals, salts, solvates, polymorphs. However, utilization this important technique synthesis pharmaceutically biologically relevant targets was not adequately investigated. This review article summarizes overview latest development LAG approaches active pharmaceutical ingredients (API) drug‐like fragments, highlights superiority versus conventional syntheses. magnified image

Language: Английский

Citations

253

Mechanochemistry: New Tools to Navigate the Uncharted Territory of “Impossible” Reactions DOI Creative Commons
Federico Cuccu, Lidia De Luca, Francesco Delogu

et al.

ChemSusChem, Journal Year: 2022, Volume and Issue: 15(17)

Published: July 21, 2022

Mechanochemical transformations have made chemists enter unknown territories, forcing a different chemistry perspective. While questioning or revisiting familiar concepts belonging to solution chemistry, mechanochemistry has broken new ground, especially in the panorama of organic synthesis. Not only does it foster "thinking outside box", but also opened reaction paths, allowing overcome weaknesses traditional exactly where use well-established solution-based methodologies rules out progress. In this Review, reader is introduced an intriguing research subject not yet fully explored and waiting for improved understanding. Indeed, study mainly focused on that, although impossible solution, become possible under mechanochemical processing conditions, simultaneously entailing innovation expanding chemical space.

Language: Английский

Citations

193

Tribochemistry, Mechanical Alloying, Mechanochemistry: What is in a Name? DOI Creative Commons
Adam A. L. Michalchuk∞, E.V. Boldyreva, Ana M. Belenguer

et al.

Frontiers in Chemistry, Journal Year: 2021, Volume and Issue: 9

Published: May 26, 2021

Over the decades, application of mechanical force to influence chemical reactions has been called by various names: mechanochemistry, tribochemistry, alloying, name but a few. The evolution these terms largely mirrored understanding field. But what is meant terms, why have they evolved, and does it really matter how process called? Which parameters should be defined describe unambiguously experimental conditions such that others can reproduce results, or allow meaningful comparison between processes explored under different conditions? Can information on encoded in clear, concise, self-explanatory way? We address questions this Opinion contribution, which we hope will spark timely constructive discussion across international mechanochemical community.

Language: Английский

Citations

165

Continuous flow mechanochemistry: reactive extrusion as an enabling technology in organic synthesis DOI Creative Commons
Robert R. A. Bolt, Jamie A. Leitch, Andrew C. Jones

et al.

Chemical Society Reviews, Journal Year: 2022, Volume and Issue: 51(11), P. 4243 - 4260

Published: Jan. 1, 2022

Reactive extrusion provides a scale-up opportunity to turn mechanochemical process from ball-mill into continuous flow. This tutorial review summarises some of the early ground-breaking work in this area.

Language: Английский

Citations

116

Upscaling Mechanochemistry: Challenges and Opportunities for Sustainable Industry DOI Creative Commons
Evelina Colacino, Valerio Isoni, Deborah E. Crawford

et al.

Trends in Chemistry, Journal Year: 2021, Volume and Issue: 3(5), P. 335 - 339

Published: March 27, 2021

Language: Английский

Citations

106

Green metrics in mechanochemistry DOI Creative Commons

Nicolas Fantozzi,

Jean‐Noël Volle, Andrea Porcheddu

et al.

Chemical Society Reviews, Journal Year: 2023, Volume and Issue: 52(19), P. 6680 - 6714

Published: Jan. 1, 2023

The quantitative assessment of the greenness mechanochemical processes for green metrics were calculated is herein reported. A general introduction to topic, variables influencing reaction outcome and, an outlook are also provided.

Language: Английский

Citations

89

Mechanochemistry Can Reduce Life Cycle Environmental Impacts of Manufacturing Active Pharmaceutical Ingredients DOI
Or Galant,

Giacomo Cerfeda,

Aaron S. McCalmont

et al.

ACS Sustainable Chemistry & Engineering, Journal Year: 2022, Volume and Issue: 10(4), P. 1430 - 1439

Published: Jan. 20, 2022

The scale-up of mechanochemical methods could play a transformative role in making manufacturing processes the pharmaceutical industry greener by eliminating solvent use and recovery. Combined with energy-efficient continuous processing that consolidates reaction steps, mechanochemistry's environmental economic benefits may translate across product supply chains. Here, we evaluate numerous sustainability green chemistry metrics for producing nitrofurantoin, an active ingredient (API), via twin-screw extrusion (TSE) conventional solvent-batch synthesis methods. We find significant reduction all TSE including energy, climate change, human ecological health, as well cost due to reducing excess reactant consumption solvents while maintaining high selectivity. In addition, replacing direct energy source drive chemical from mostly thermal electrical sources does not increase net life cycle consumed produce functionally equivalent API. conclude holds multiple APIs potentially other products.

Language: Английский

Citations

88

Salient Achievements in Synthetic Organic Chemistry Enabled by Mechanochemical Activation DOI
Eusebio Juaristi, C.G. Ávila-Ortíz

Synthesis, Journal Year: 2023, Volume and Issue: 55(16), P. 2439 - 2459

Published: May 3, 2023

Abstract Although known for millennia, it is only recently that mechanochemistry has received serious attention by chemists. Indeed, during the past 15 years an extraordinary number of reports concerning solid-state chemical transformations through grinding and milling techniques have been recorded. This short review discusses circumstances led this renaissance, highlighting present intense interest in so-called green chemistry, enabling capacity to handle insoluble substrates, identification profound influence additives can on mechanochemically activated reactions. The core account focuses salient developments synthetic organic especially amino acid peptide­ mechanosynthesis, successful employment mechanochemical activation combination with asymmetric organocatalysis, promising enzymatic whole cell biocatalysis, remarkable achievement multicomponent selective reactions via complex, multistep reaction pathways, mechanosynthesis representative heterocycles. final section comments some pending tasks area, such as scaling-up processes be practical use industry, requirement easier more efficient control parameters monitoring devices, consequently careful analysis additional procedures a proper understanding phenomena. 1 Introduction 2 Brief History Mechanochemistry 3 Milling Equipment Reaction Parameters 4 Attributes That Propelled Its Present Renaissance 4.1 Enormous Attention Being Presently Paid Sustainable Chemistry 4.2 Reduced Energy Consumption 4.3 Additive-Based 4.4 Handling Insoluble Reactants 4.5 ‘Impossible’ Reactions Are Successful 4.6 Air- Water-Sensitive Reagents Ball 5 Salient Developments Mechanochemical Activation Synthetic Organic 5.1 Amino Acid Peptide Mechanosynthesis 5.2 Asymmetric Synthesis Organocatalysis under Ball-Milling Conditions 5.3 Mechanoenzymology 5.4 Multicomponent Activated 5.5 Heterocycles Modification 6 Future Directions 6.1 Scaling-Up Protocols 6.2 Temperature-Controlled 6.3 Understanding Transformations 6.4 Emerging Techniques 7 Conclusions

Language: Английский

Citations

52

Tinkering with Mechanochemical Tools for Scale Up DOI Creative Commons
Javier F. Reynes, Valerio Isoni, Felipe Garcı́a

et al.

Angewandte Chemie International Edition, Journal Year: 2023, Volume and Issue: 62(44)

Published: April 28, 2023

Mechanochemistry provides an environmentally benign platform to develop more sustainable chemical processes by limiting raw materials, energy use, and waste generation while using physically smaller equipment. A continuously growing research community has steadily showcased examples of beneficial mechanochemistry applications at both the laboratory preparative scale. In contrast solution-based chemistry, mechanochemical have not yet been standardized, thus scaling up is still a nascent discipline. The purpose this Minireview highlight similarities, differences challenges various approaches that successfully applied for range scales. We hope provide discussion starting point those interested in further developing commercial use and/or industrialisation.

Language: Английский

Citations

51