Cryptophycin unit B analogues

• Thomas Schachtsiek,
• Jona Voss,
• Maren Hamsen,
• Beate Neumann,
• Hans-Georg Stammler and
• Norbert Sewald

Beilstein J. Org. Chem. 2025, 21, 526–532, doi:10.3762/bjoc.21.40

• would like to thank Carmela Michalek for conducting cellular proliferation assays. Funding J.V. thanks the German National Academic Foundation (Studienstiftung des deutschen Volkes) for a scholarship.

Efficient synthesis of fluorinated triphenylenes with enhanced arene–perfluoroarene interactions in columnar mesophases

• Yang Chen,
• Jiao He,
• Hang Lin,
• Hai-Feng Wang,
• Ping Hu,
• Bi-Qin Wang,
• Ke-Qing Zhao and
• Bertrand Donnio

Beilstein J. Org. Chem. 2024, 20, 3263–3273, doi:10.3762/bjoc.20.270

• Yang Chen Jiao He Hang Lin Hai-Feng Wang Ping Hu Bi-Qin Wang Ke-Qing Zhao Bertrand Donnio College of Chemistry and Materials Science, Sichuan Normal University, Chengdu 610066, China Institut de Physique et Chimie des Matériaux de Strasbourg (IPCMS), CNRS-Université de Strasbourg (UMR 7504), F

Synthesis of extended fluorinated tripeptides based on the tetrahydropyridazine scaffold

• Thierry Milcent,
• Pascal Retailleau,
• Benoit Crousse and
• Sandrine Ongeri

Beilstein J. Org. Chem. 2024, 20, 3174–3181, doi:10.3762/bjoc.20.262

• Thierry Milcent Pascal Retailleau Benoit Crousse Sandrine Ongeri UMR 8076, BioCIS, CNRS, Université Paris-Saclay, avenue des sciences, 91400 Orsay, France Université Paris-Saclay, CNRS, Institut de Chimie des Substances Naturelles, 91198 Gif-sur-Yvette, France 10.3762/bjoc.20.262 Abstract The

Synthesis and cytotoxicity studies of novel N-arylbenzo[h]quinazolin-2-amines

• Battini Veeraiah,
• Kishore Ramineni,
• Dabbugoddu Brahmaiah,
• Nangunoori Sampath Kumar,
• Hélène Solhi,
• Rémy Le Guevel,
• Chada Raji Reddy,
• Frédéric Justaud and
• René Grée

Beilstein J. Org. Chem. 2024, 20, 2592–2598, doi:10.3762/bjoc.20.218

• , India Univ Rennes, Plateform ImPACcell, BIOSIT, F-35000 Rennes, France CSIR-Indian Institute of Chemical Technology, Uppal Road, Tarnaka, Hyderabad 500007, TS, India Univ Rennes, CNRS, ISCR (Institut des Sciences Chimiques de Rennes), UMR 6226, F-35000 Rennes, France 10.3762/bjoc.20.218 Abstract In

Hypervalent iodine-mediated cyclization of bishomoallylamides to prolinols

• Smaher E. Butt,
• Konrad Kepski,
• Jean-Marc Sotiropoulos and
• Wesley J. Moran

Beilstein J. Org. Chem. 2024, 20, 2455–2460, doi:10.3762/bjoc.20.209

• Smaher E. Butt Konrad Kepski Jean-Marc Sotiropoulos Wesley J. Moran Department of Physical and Life Sciences, University of Huddersfield, Queensgate, Huddersfield HD1 3DH, United Kingdom Université de Pau et des Pays de l’Adour, IPREM (CNRS-UMR 5254), Technopole Hélioparc, 2 Avenue du Président

• des Pays de l’Adour for access to their computer cluster.

Improved deconvolution of natural products’ protein targets using diagnostic ions from chemical proteomics linkers

• Andreas Wiest and
• Pavel Kielkowski

Beilstein J. Org. Chem. 2024, 20, 2323–2341, doi:10.3762/bjoc.20.199

• FragPipe (B) in case of the adamantane-based probe from the study by Wozniak et al. [110]. An alternative DADPS linker. Chemical structure of the trifunctional trypsin cleavable AzKTB linker. Funding This work was funded by a Ph.D. fellowship from the Studienstiftung des deutschen Volkes to A.W. and a

Cell-free protein synthesis with technical additives – expanding the parameter space of in vitro gene expression

• Tabea Bartsch,
• Stephan Lütz and
• Katrin Rosenthal

Beilstein J. Org. Chem. 2024, 20, 2242–2253, doi:10.3762/bjoc.20.192

• some of the gaps in the consideration of the general physical properties and potential effects on the performance of Escherichia coli-based CFPS. We use technical additives, such as water-soluble macromolecular polymers and salts, which are commonly used as deep eutectic solvents (DES) and extend the

• influence on the synthesis performance of CFPS. Polymers, DES, and organic solvents were considered to modify the fluid properties. Polymers and deep eutectic solvents (DES) as additives in CFPS Polymers (PEG, methylcellulose (MC), and carboxymethylcellulose (CMC)) and DES (choline chloride/urea, betaine

• /ethylene glycol (EG), and choline chloride/glycerol) were chosen as additives to vary the viscosity, ion concentration, amount of macromolecules, and osmolarity in CFPS. The calculated values for the properties of the CFPS system with polymers and DES added at different concentrations are shown in Table 1

Electrochemical allylations in a deep eutectic solvent

• Sophia Taylor and
• Scott T. Handy

Beilstein J. Org. Chem. 2024, 20, 2217–2224, doi:10.3762/bjoc.20.189

• (DES) were reported and have been heavily promoted as cost-effective replacements for RTILs in many applications [17][18]. One of the early and very effective applications of DES was in the area of electroplating as well as metal recovery by electrodeposition [19]. Despite this fascinating potential

• , very little has been reported in terms of their use in electrosynthesis [20][21][22][23][24]. Given our interest in both electrosynthesis and DES, we opted to explore this combination in the area of electrochemical allylation. The allylation of carbonyls is a valuable reaction that has been explored

• under a wide range of conditions, including several reports using electrochemical conditions [25][26]. Recently, an allylation in DES has also been reported, but using indium as the reducing metal under standard Barbier-type conditions, but not electrochemical ones [27]. While the unusual DES

Factors influencing the performance of organocatalysts immobilised on solid supports: A review

• Zsuzsanna Fehér,
• Dóra Richter,
• Gyula Dargó and
• József Kupai

Beilstein J. Org. Chem. 2024, 20, 2129–2142, doi:10.3762/bjoc.20.183

• -nitrostyrene, the recyclability of the organocatalyst in the betaine/sorbitol/water DES system was demonstrated up to 10 cycles without any significant decrease in yield (up to 99%) or stereoselectivity (up to 96% ee). Encapsulation is an irreversible method and the only catalyst immobilisation process that

Multicomponent syntheses of pyrazoles via (3 + 2)-cyclocondensation and (3 + 2)-cycloaddition key steps

• Ignaz Betcke,
• Alissa C. Götzinger,
• Maryna M. Kornet and
• Thomas J. J. Müller

Beilstein J. Org. Chem. 2024, 20, 2024–2077, doi:10.3762/bjoc.20.178

• solvents (DES) [83]. Catalysis can also be achieved using molecular iodine [84], AlCl3 [85], sodium ascorbate [86], and even solid-state and nanoparticle-mediated catalysts like CuO/ZrO2 [87], Fe3O4@Si@MoO2 [88], caspacin-cyclodextrin functionalized magnetite nanoparticles (CPS CD) [89], and Mg-Fe

Harnessing the versatility of hydrazones through electrosynthetic oxidative transformations

• Aurélie Claraz

Beilstein J. Org. Chem. 2024, 20, 1988–2004, doi:10.3762/bjoc.20.175

• Aurelie Claraz Institut de Chimie des Substances Naturelles, CNRS, Univ. Paris-Saclay, 1 Avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France 10.3762/bjoc.20.175 Abstract Hydrazones are important structural motifs in organic synthesis, providing a useful molecular platform for the

Syntheses and medicinal chemistry of spiro heterocyclic steroids

• Laura L. Romero-Hernández,
• Ana Isabel Ahuja-Casarín,
• Penélope Merino-Montiel,
• Sara Montiel-Smith,
• José Luis Vega-Báez and
• Jesús Sandoval-Ramírez

Beilstein J. Org. Chem. 2024, 20, 1713–1745, doi:10.3762/bjoc.20.152

• cyclopamine. Comparing the biological results of the compound with the activity of desmethylveramiline (a des-E analogue of cyclopamine) has suggested that the rigidity of the oxetane ring is crucial for the potency of compound 7 [12]. Spiro-β-lactone steroids Beller et al. reported a selective method for

Advancements in hydrochlorination of alkenes

• Daniel S. Müller

Beilstein J. Org. Chem. 2024, 20, 787–814, doi:10.3762/bjoc.20.72

• Daniel S. Muller Univ. Rennes, CNRS, ISCR (Institut des Sciences Chimiques de Rennes) – UMR 6226, 263 Avenue du Général Leclerc, F-35000 Rennes, France 10.3762/bjoc.20.72 Abstract The hydrochlorination of alkenes has been extensively studied in research and is commonly featured in organic

Green and sustainable approaches for the Friedel–Crafts reaction between aldehydes and indoles

• Periklis X. Kolagkis,
• Eirini M. Galathri and
• Christoforos G. Kokotos

Beilstein J. Org. Chem. 2024, 20, 379–426, doi:10.3762/bjoc.20.36

Synthesis of π-conjugated polycyclic compounds by late-stage extrusion of chalcogen fragments

• Aissam Okba,
• Pablo Simón Marqués,
• Kyohei Matsuo,
• Naoki Aratani,
• Hiroko Yamada,
• Gwénaël Rapenne and
• Claire Kammerer

Beilstein J. Org. Chem. 2024, 20, 287–305, doi:10.3762/bjoc.20.30

Thienothiophene-based organic light-emitting diode: synthesis, photophysical properties and application

• Recep Isci and
• Turan Ozturk

Beilstein J. Org. Chem. 2023, 19, 1849–1857, doi:10.3762/bjoc.19.137

• adapted with permission of Institution of Chemical Engineers (IChemE) and The Royal Society of Chemistry from [38] (“Cationic and radical polymerization using a boron–thienothiophene–triphenylamine based D-π-A type photosensitizer under white LED irradiation”) by A. Suerkan et al., Mol. Syst. Des. Eng

Synthesis of 5-arylidenerhodanines in L-proline-based deep eutectic solvent

• Stéphanie Hesse

Beilstein J. Org. Chem. 2023, 19, 1537–1544, doi:10.3762/bjoc.19.110

• scaffolds is the introduction of a benzylidene moiety on C5 via a Knoevenagel reaction. Here, a facile synthesis of 5-arylidenerhodanines via a Knoevenagel reaction in an ʟ-proline-based deep eutectic solvent (DES) is reported. This method is fast (1 h at 60 °C), easy, catalyst-free and sustainable as no

• compounds are the more active ones. Keywords: antioxidant; deep eutectic solvent; Knoevenagel; ʟ-proline DES; rhodanine; Introduction Rhodanines and related five-membered heterocycles with multiple heteroatoms (i.e., thiazolidinediones, thiazolidinones, hydantoins, thiohydantoins) are very interesting

• , volatile solvents, hard conditions, and/or difficult purifications. However, green chemistry has become a crucial sub-discipline in the field of chemistry and the chemical industry is giving major priority to sustainable processes. Since a few years, deep eutectic solvents (DES) are considered as a

Clauson–Kaas pyrrole synthesis using diverse catalysts: a transition from conventional to greener approach

• Dileep Kumar Singh and
• Rajesh Kumar

Beilstein J. Org. Chem. 2023, 19, 928–955, doi:10.3762/bjoc.19.71

• bond donating groups were investigated. Among these, the DES prepared by mixing quaternary ammonium salts choline chloride (ChCl) and the hydrogen-bond donor L-(+)-tartaric acid gives the best result. Moreover, L-(+)-tartaric acid–ChCl acts as both solvent and catalyst for pyrrole synthesis. This

• interaction between DES and the amino group enhance the nucleophlicity of the amines. (3) Microwave-assisted reactions Microwave-assisted heating offers a number of advantages over conventional heating, such as greater precision, excellent product yields, and very rapid reaction. This section describes the

Mechanochemical solid state synthesis of copper(I)/NHC complexes with K₃PO₄

• Ina Remy-Speckmann,
• Birte M. Zimmermann,
• Mahadeb Gorai,
• Martin Lerch and
• Johannes F. Teichert

Beilstein J. Org. Chem. 2023, 19, 440–447, doi:10.3762/bjoc.19.34

• Ina Remy-Speckmann Birte M. Zimmermann Mahadeb Gorai Martin Lerch Johannes F. Teichert Institut für Chemie, Technische Universität Berlin, Straße des 17. Juni 115, 10623 Berlin, Germany Fakultät für Naturwissenschaften, Technische Universität Chemnitz, Straße der Nationen 62, 09111 Chemnitz

Sequential hydrozirconation/Pd-catalyzed cross coupling of acyl chlorides towards conjugated (2E,4E)-dienones

• Benedikt Kolb,
• Daniela Silva dos Santos,
• Sanja Krause,
• Anna Zens and
• Sabine Laschat

Beilstein J. Org. Chem. 2023, 19, 176–185, doi:10.3762/bjoc.19.17

• ), the Ministerium für Wissenschaft, Forschung und Kunst des Landes Baden-Württemberg, the Fonds der Chemischen Industrie, the Merck KGaA, Darmstadt, is gratefully acknowledged.

Total synthesis of grayanane natural products

• Nicolas Fay,
• Rémi Blieck,
• Cyrille Kouklovsky and
• Aurélien de la Torre

Beilstein J. Org. Chem. 2022, 18, 1707–1719, doi:10.3762/bjoc.18.181

• Nicolas Fay Remi Blieck Cyrille Kouklovsky Aurelien de la Torre Institut de Chimie Moléculaire et des Matériaux d’Orsay (ICMMO), Université Paris-Saclay, CNRS, 15, rue Georges Clémenceau, 91405 Orsay Cedex, France 10.3762/bjoc.18.181 Abstract Grayananes are a broad family of diterpenoids found in

Preparation of an advanced intermediate for the synthesis of leustroducsins and phoslactomycins by heterocycloaddition

• Anaïs Rousseau,
• Guillaume Vincent and
• Cyrille Kouklovsky

Beilstein J. Org. Chem. 2022, 18, 1385–1395, doi:10.3762/bjoc.18.143

• Anais Rousseau Guillaume Vincent Cyrille Kouklovsky Institut de Chimie Moléculaire et des Matériaux d’Orsay, Université Paris-Saclay, CNRS, F-91405 Orsay, France 10.3762/bjoc.18.143 Abstract A convergent strategy for the synthesis of leustroducsins and phoslactomycins has been designed, relying

On drug discovery against infectious diseases and academic medicinal chemistry contributions

• Yves L. Janin

Beilstein J. Org. Chem. 2022, 18, 1355–1378, doi:10.3762/bjoc.18.141

• Yves L. Janin Structure et Instabilité des Génomes (StrInG), Muséum National d'Histoire Naturelle, INSERM, CNRS, Alliance Sorbonne Université, 75005 Paris, France 10.3762/bjoc.18.141 Abstract This perspective is an attempt to document the problems that medicinal chemists are facing in drug

On Reuben G. Jones synthesis of 2-hydroxypyrazines

• Pierre Legrand and
• Yves L. Janin

Beilstein J. Org. Chem. 2022, 18, 935–943, doi:10.3762/bjoc.18.93

• Pierre Legrand Yves L. Janin Synchrotron SOLEIL, L'Orme des Merisiers, 91190 Saint-Aubin, France Structure et Instabilité des Génomes (StrInG), Muséum National d'Histoire Naturelle, INSERM, CNRS, Alliance Sorbonne Université, 75005 Paris, France 10.3762/bjoc.18.93 Abstract In 1949, Reuben G

Correction: Amine–borane complex-initiated SF₅Cl radical addition on alkenes and alkynes

• Audrey Gilbert,
• Pauline Langowski,
• Marine Delgado,
• Laurent Chabaud,
• Mathieu Pucheault and
• Jean-François Paquin

Beilstein J. Org. Chem. 2021, 17, 1725–1726, doi:10.3762/bjoc.17.120

• Audrey Gilbert Pauline Langowski Marine Delgado Laurent Chabaud Mathieu Pucheault Jean-Francois Paquin Départment de chimie, Université Laval, Québec, QC, G1V 0A6, Canada Institut des Sciences Moléculaires - Groupe ORGA - UMR 5255, Université de Bordeaux, 351 Cours de la libération, 33405 Talence