Metal-catalyzed coupling/carbonylative cyclizations for accessing dibenzodiazepinones: an expedient route to clozapine and other drugs

• Amina Moutayakine and
• Anthony J. Burke

Beilstein J. Org. Chem. 2024, 20, 193–204, doi:10.3762/bjoc.20.19

• suitable surrogate. Not only that, the use of safer to use surrogates, is important for use in enabling technologies, like continuous flow and microwave-heated reactions. In fact, CO-free aminocarbonylation reactions are well known, and molybdenum hexacarbonyl (Mo(CO)6) is a very useful surrogate having

Inductive heating and flow chemistry – a perfect synergy of emerging enabling technologies

• Conrad Kuhwald,
• Sibel Türkhan and
• Andreas Kirschning

Beilstein J. Org. Chem. 2022, 18, 688–706, doi:10.3762/bjoc.18.70

• chemistry, but also in medicine. Traditionally, inductive heating is used in industry, e.g., for heating large metallic objects including bending, bonding, and welding pipes. In addition, inductive heating has emerged as a partner for flow chemistry, both of which are enabling technologies for organic

• synthesis. This report reviews the combination of flow chemistry and inductive heating in industrial settings as well as academic research and demonstrates that the two technologies ideally complement each other. Keywords: catalysis; enabling technologies; flow chemistry; inductive heating; multistep

• of continuously operated chemical processes with induction heating for the fields of bulk chemical production and the fragrance and flavor industries, as well as, eventually, the pharmaceutical industry. The authors are certain that this combination of enabling technologies holds great future

Flow synthesis of oxadiazoles coupled with sequential in-line extraction and chromatography

• Kian Donnelly and
• Marcus Baumann

Beilstein J. Org. Chem. 2022, 18, 232–239, doi:10.3762/bjoc.18.27

• telescoping; Introduction The application of enabling technologies in chemistry has received a surge in interest in recent years [1][2][3][4]. At the forefront of this revolution has been the advent of flow chemistry and its increasing utility in synthetic chemistry [5][6][7][8]. This is largely driven by

A comprehensive review of flow chemistry techniques tailored to the flavours and fragrances industries

• Guido Gambacorta,
• James S. Sharley and
• Ian R. Baxendale

Beilstein J. Org. Chem. 2021, 17, 1181–1312, doi:10.3762/bjoc.17.90

A sustainable strategy for the straightforward preparation of 2H-azirines and highly functionalized NH-aziridines from vinyl azides using a single solvent flow-batch approach

• Michael Andresini,
• Leonardo Degannaro and
• Renzo Luisi

Beilstein J. Org. Chem. 2021, 17, 203–209, doi:10.3762/bjoc.17.20

• risks [6]. Recently, a variety of sustainable solvents has been therefore identified, and their use have been combined with those of enabling technologies. In this scenario, the development of continuous flow synthetic methodologies has found its fortune in the past two decades [7][8][9]. Several

• to the large surface–volume ratio of microreactors, and may prevent the formation of undesirable byproducts that are not avoidable under the traditional batch conditions. As a consequence, efforts have been devoted to the development of synthetic processes combining GCP and enabling technologies [11

Recent applications of porphyrins as photocatalysts in organic synthesis: batch and continuous flow approaches

• Rodrigo Costa e Silva,
• Luely Oliveira da Silva,
• Aloisio de Andrade Bartolomeu,
• Timothy John Brocksom and
• Kleber Thiago de Oliveira

Beilstein J. Org. Chem. 2020, 16, 917–955, doi:10.3762/bjoc.16.83

• conjugated photosensitizers show increasing potential in photocatalysis since they combine both photo- and electrochemical properties which can substitute available metalloorganic photocatalysts. Batch and continuous-flow approaches are presented highlighting the relevance of enabling technologies for the

Back to the future: Why we need enzymology to build a synthetic metabolism of the future

• Tobias J. Erb

Beilstein J. Org. Chem. 2019, 15, 551–557, doi:10.3762/bjoc.15.49

• is beyond any doubt that synthetic chemistry has been one of the key enabling technologies of the 20th century, which has virtually changed the world we are living in. Biology is currently at the verge of a similar transition [5]. Over the last decades, our ability to analyze and manipulate living

NMR reaction monitoring in flow synthesis

• M. Victoria Gomez and
• Antonio de la Hoz

Beilstein J. Org. Chem. 2017, 13, 285–300, doi:10.3762/bjoc.13.31

• optimization is discussed. Keywords: expert systems; flow chemistry; microcoil; NMR probes; Introduction New enabling technologies have facilitated the transition from traditional chemistry to a more automated approach that will be the chemistry of the 21st century [1][2]. The objective is that the reaction

• the small amounts of reagents and the use of a closed system with efficient control of pressure. The use of solvents can be minimized since concentrations can be increased up to the limit of solubility. Coupling with other enabling technologies is very simple and more efficient than in batch

Superstructures with cyclodextrins: chemistry and applications III

• Gerhard Wenz and
• Eric Monflier

Beilstein J. Org. Chem. 2016, 12, 937–938, doi:10.3762/bjoc.12.91

• highly dangerous substances to be trapped and hydrolyzed before they reach their biological target. G. Cravotto et al. have reported on the recent advances in enabling technologies and green processes in CD chemistry [15]. By increasing heat and mass transfer, the protocols (assisted by microwaves

Enabling technologies and green processes in cyclodextrin chemistry

• Giancarlo Cravotto,
• Marina Caporaso,
• Laszlo Jicsinszky and
• Katia Martina

Beilstein J. Org. Chem. 2016, 12, 278–294, doi:10.3762/bjoc.12.30

• green strategies for the selective modification of cyclodextrins (CDs) is still a challenging task. Outstanding results have been achieved in recent years by means of so-called enabling technologies, such as microwaves, ultrasound and ball mills, that have become irreplaceable tools in the synthesis of

• ; cyclodextrin; microwaves; synthesis; ultrasound; Review The last decade has witnessed the development of highly efficient alternative synthetic methods which make use of new enabling technologies. The need for a more rational approach to the synthesis of cyclodextrin (CD) derivatives has led to several energy

• highlight the huge advantages and potential scalability of these so-called enabling technologies that maximize heat and mass transfer. Although many advances have been made during the past decade, the most exciting results in this field are surely yet to come. Ultrasound US irradiation is an environmentally

The synthesis of active pharmaceutical ingredients (APIs) using continuous flow chemistry

• Marcus Baumann and
• Ian R. Baxendale

Beilstein J. Org. Chem. 2015, 11, 1194–1219, doi:10.3762/bjoc.11.134

• : continuous processing; flow synthesis; in-line analysis; manufacture; pharmaceuticals; scalability; Introduction The last 20 years have witnessed a true renaissance in the way synthetic chemistry is performed due to the implementation of various enabling technologies allowing the modern synthesis chemist to

• . Arguably one of the most widely amenable of the enabling technologies is flow chemistry, which accommodates small foot-print reactors in which streams of substrates and reagents can be united to react in a highly controlled and reproducible environment [7][8][9][10][11][12][13][14][15]. Importantly

• synthesis of a complex molecule. However, despite the successful completion of this campaign, it could be argued that the development time required for such a complex molecule in flow can be protracted; therefore both synthetic route and available enabling technologies should be carefully examined before

An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles

• Marcus Baumann and
• Ian R. Baxendale

Beilstein J. Org. Chem. 2013, 9, 2265–2319, doi:10.3762/bjoc.9.265

• outlay [5]. As a result pharmaceutical companies are constantly seeking ways to accelerate this development process by adopting new synthetic methodologies and enabling technologies in order to profitably generate new medications for both old and new targets [6]. By reviewing the synthetic routes used to

The application of a monolithic triphenylphosphine reagent for conducting Ramirez gem-dibromoolefination reactions in flow

• Kimberley A. Roper,
• Malcolm B. Berry and
• Steven V. Ley

Beilstein J. Org. Chem. 2013, 9, 1781–1790, doi:10.3762/bjoc.9.207

• using monolithic supports over traditional beads in flow chemistry protocols can greatly facilitate the synthesis of fine chemicals using these enabling technologies [36]. We have recently reported on the development of a monolithic triphenylphosphine reagent and its application to the Staudinger aza

The rapid generation of isothiocyanates in flow

• Marcus Baumann and
• Ian R. Baxendale

Beilstein J. Org. Chem. 2013, 9, 1613–1619, doi:10.3762/bjoc.9.184

• still seen and there normally remains the requirement for time consuming purifications such as column chromatography in order to isolate pure products. Immobilised reagents have shown great promise as enabling technologies when incorporated in flow reactors to aid in the processing, work-up and

Camera-enabled techniques for organic synthesis

• Steven V. Ley,
• Richard J. Ingham,
• Matthew O’Brien and
• Duncan L. Browne

Beilstein J. Org. Chem. 2013, 9, 1051–1072, doi:10.3762/bjoc.9.118

• other enabling technologies [16][33][34][35] are receiving increased attention. With the continuing development of digital imaging technology, computer vision techniques and laboratory automation, some of these routine tasks may be delegated to a computer. Not only will this allow skilled researchers to

• area in which enabling technologies make a significant impact is when a process is taken from the laboratory to an industrial scale. In a recent publication by Kadam and co-workers [67] a number of process analytical technologies (PAT), including visual monitoring of the crystal size and shape

Automated three-component synthesis of a library of γ-lactams

• Erik Fenster,
• David Hill,
• Oliver Reiser and
• Jeffrey Aubé

Beilstein J. Org. Chem. 2012, 8, 1804–1813, doi:10.3762/bjoc.8.206

• as pharmacological probes and as starting points for drug-discovery campaigns, has primarily fuelled this interest, while enabling technologies, such as diversity-oriented synthesis (DOS), have improved access to small-molecule libraries [1][2][3][4][5]. Compounds containing a γ-lactam moiety have

Translation of microwave methodology to continuous flow for the efficient synthesis of diaryl ethers via a base-mediated S_NAr reaction

• Charlotte Wiles and
• Paul Watts

Beilstein J. Org. Chem. 2011, 7, 1360–1371, doi:10.3762/bjoc.7.160

• = 195 °C). Graphical representation of an automated flow reaction for equilibration and screening of reactor temperature effects. Illustration of the model reaction used to compare the enabling technologies of microwave and microreactor synthesis. Illustration of the model reaction used to benchmark

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

• Marcus Baumann,
• Ian R. Baxendale,
• Steven V. Ley and
• Nikzad Nikbin

Beilstein J. Org. Chem. 2011, 7, 442–495, doi:10.3762/bjoc.7.57

Flow through reactors for organic chemistry: directly electrically heated tubular mini reactors as an enabling technology for organic synthesis

• Ulrich Kunz and
• Thomas Turek

Beilstein J. Org. Chem. 2009, 5, No. 70, doi:10.3762/bjoc.5.70

• operated mini reactor for chemical reactions using readily available laboratory equipment. In this sense it is an enabling technology allowing the use of continuous reactors at low cost, enlarging the portfolio of enabling technologies for organic synthesis [27]. Performing a simple organic reaction