Recent advances in copper-catalyzed direct hydroamination of alkenes with (hetero)aromatic amines

• Hyejeong Lee and
• Yunmi Lee

Beilstein J. Org. Chem. 2026, 22, 925–947, doi:10.3762/bjoc.22.73

• characterization of well-defined copper–amido complexes I and II, supported by electron-donating ligands such as phosphines and N-heterocyclic carbenes (NHCs) (Scheme 2) [32][33][34]. Copper–amido complex I was prepared by treating the dtbpe-ligated Cu–Cl complex (dtbpe = 1,2-bis(di-tert-butylphosphino)ethane

A practical CO₂-mediated synthesis of 5,6-carboxylated silicon-rhodamines for targeted probe development

• Dongjie Hou,
• Shaowei Wu,
• Ning Xu,
• Pengjun Bao,
• Wenhao Jia,
• Qinglong Qiao and
• Zhaochao Xu

Beilstein J. Org. Chem. 2026, 22, 915–924, doi:10.3762/bjoc.22.72

• with 4c in live HeLa cells. Scale bars: 5.0 μm. Supporting Information Supporting Information File 8: Experimental details and characterization of compounds by NMR and ESIMS. Funding This work is supported by the National Natural Science Foundation of China (22541705, U25A20620, 22225806, 22522816

Cascade transformation of 2-(diazoacetyl)-2H-azirines to 2-aroyl-3-hydroxy-1H-pyrroles via condensation with aromatic aldehydes

• Timur O. Zanakhov,
• Ekaterina E. Galenko,
• Mikhail S. Novikov and
• Alexander F. Khlebnikov

Beilstein J. Org. Chem. 2026, 22, 897–904, doi:10.3762/bjoc.22.70

• Crystallographic Data Centre. Supporting Information File 3: Full experimental details, characterization data and copies of NMR spectra for all new compounds. Supporting Information File 4: Crystallographic information file for compound 5a. Acknowledgements This research was carried out using resources of the

Chiral cyclopropenimine-catalyzed enantioselective Michael reactions of phenol and benzofuran-derived α,β-unsaturated pyrazolamides with benzophenone-imine of glycine esters

• Ya Bai,
• Xue-Ying Wang,
• Si-Kai Zhu,
• Yan-Ting Shen,
• Sheng-Yong Zhang and
• Ping-An Wang

Beilstein J. Org. Chem. 2026, 22, 888–896, doi:10.3762/bjoc.22.69

• Supporting Information File 42: Detailed experimental procedures, characterization data of all new compounds with NMR, HRMS, HPLC charts, and X-ray single crystal diffraction data. Funding The authors thank the National Science Foundation of China (no. 21372259) for providing financial support for this work.

Diastereodivergent electrophilic trapping of α-boryl lithium derivatives

• Tereza Pavlíčková,
• Noam Orbach and
• Ilan Marek

Beilstein J. Org. Chem. 2026, 22, 882–887, doi:10.3762/bjoc.22.68

• File 40: Experimental section, characterization data and copies of spectra. Funding This project has received funding from the European Union’s Horizon 2020 Research and Innovation Program, under Grant Agreement No. 101198411, from the Israel Science Foundation administered by the Israel Academy of

Unsymmetrical sulfoxides with sterically hindered catechol fragment: synthesis, structure, electrochemical properties, and antiradical activity

• Daria A. Burmistrova,
• Vasiliy A. Fokin,
• Oleg P. Demidov,
• Mikhail A. Kiskin,
• Maxim V. Arsenyev,
• Andrey I. Poddel’sky,
• Nadezhda T. Berberova and
• Ivan V. Smolyaninov

Beilstein J. Org. Chem. 2026, 22, 828–837, doi:10.3762/bjoc.22.65

• . Supporting Information Supporting Information File 37: Experimental procedures and characterization data. Supporting Information File 38: Crystallographic information files. Funding This work was supported by the Russian Science Foundation, grant 25-73-00164.

Synthetic study of vic-bromination of diarylacetylenes, easy purification and separation

• Akane Togo,
• Hiyono Suzuki,
• Yuto Akai,
• Makoto Matsumoto,
• Yoshinori Suzuma,
• Hidehiko Kodama and
• Kouichi Matsumoto

Beilstein J. Org. Chem. 2026, 22, 795–802, doi:10.3762/bjoc.22.61

• contribute to process chemistry for the synthesis of (E)-1,2-dibromo-1,2-diphenylethylene and their derivatives. Further synthetic investigations are currently underway in our laboratory. Experimental The experimental procedures and characterization data (Table 1, entry 1). The glass flask was dried and

• present reaction. Reaction optimization of bromination reaction of diphenylacetylene (1a). Scope and limitations for bromination of various diarylacetylenes 1. Supporting Information Supporting Information File 24: General remarks, preparation of substrates, experimental procedure, characterization data

Halogenated azobenzene acrylates: from efficient solution photoswitching to stable solid-state photochromic materials

• Martina Vachtlová,
• Michaela Fecková,
• Vítězslav Zima,
• Jan Podlesný,
• Milan Klikar,
• Oldřich Pytela,
• Patrik Pařík,
• Jakub Opršal,
• Eliška Juhaňáková,
• Veronika Chrtová and
• Filip Bureš

Beilstein J. Org. Chem. 2026, 22, 782–794, doi:10.3762/bjoc.22.60

• . Neumanna 1316, Pardubice, 53002, Czech Republic Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentská 573, Pardubice, 53210, Czech Republic 10.3762/bjoc.22.60 Abstract The design, synthesis, and comprehensive characterization of six novel

• Information Supporting Information File 22: Experimental section, characterization data and details on compound analyses. Funding The work was supported by the Technology Agency of the Czech Republic, Sigma (project No. TQ03000624 “Photoresponsive azo-polymeric materials applied as a thermal sensor”).

Design, synthesis, and biological evaluation of FXR/ASK1 dual-target modulators

• Xi Zhang,
• Jingyan Wang,
• Ziqiang Zhao,
• Caiyi Wang,
• Zenghui Ye,
• Wei-Yuan Ma,
• Jian-Xing Xu and
• Fengzhi Zhang

Beilstein J. Org. Chem. 2026, 22, 771–781, doi:10.3762/bjoc.22.59

• study, we present the rational design and characterization of a balanced dual modulator targeting the nuclear receptors FXR and ASK1 [32], with the objective of advancing this experimental therapeutic concept (Scheme 3) [33][34]. The conception of this class of dual ligands was achieved by the merging

• Supporting Information File 20: Experimental, characterization data and copies of spectra. Funding We thank Hangzhou Medical College for financial support.

Synthesis and biological evaluation of new brassinosteroid analogs with C-22 benzoate function

• María Núñez,
• Camila Escobar,
• Mario Párraga,
• Mauricio Soto,
• Luis Espinoza-Catalán,
• Katy Díaz and
• Andrés F. Olea

Beilstein J. Org. Chem. 2026, 22, 753–762, doi:10.3762/bjoc.22.57

• characterization of new brassinosteroid (BR) analogs, in which substituents with different electronegativities and molecular sizes have been attached to a C-22 benzoate function, are described. The biological activities of all new compounds were evaluated by using the rice lamina inclination test (RLIT) and

• dihydroxylation of double bond on C-2 of compounds 23–28, following a described procedure [29], leads to BR analogs 17–22 with good reaction yields (63.4–84.9%) (Scheme 1). Structural characterization of BR analogs 17–22 was accomplished by using 13C NMR data, combined with 2D NMR techniques (HSQC and HMBC). For

Rongalite addition to dienones: diastereoselectivity in cyclic sulfone synthesis; stereochemical rationalization and prospects as a general conjugate nucleophile

• Melina Goga,
• Hao Zong,
• James Franco,
• Jazmine Prana,
• Rudolph Michel,
• Antonia Muro,
• Elana Rubin,
• Janet Brenya,
• Henk Eshuis and
• Magnus W. P. Bebbington

Beilstein J. Org. Chem. 2026, 22, 742–752, doi:10.3762/bjoc.22.56

• unknown products. Typical signals for the trans-product could be seen in the crude 1H NMR spectrum, but we were not able to isolate this compound in sufficient purity for characterization. We were intrigued to study the cyclooctanone-derived substrate 17 [41], as it would give an interesting bicyclic

Anti-invasive and cytotoxic evaluation of a (+)-pinoresinol-based semisynthetic library against glioblastoma

• Chen Zhang,
• Kah Yean Lum,
• Jonathan M. White,
• Paul I. Forster,
• Nicholas Booth,
• Sunita A. Ramesh and
• Rohan A. Davis

Beilstein J. Org. Chem. 2026, 22, 691–704, doi:10.3762/bjoc.22.54

• reported. In this study, we chemically investigated the seeds of Eremophila maculata for the first time, which led to the isolation and characterization of two known plant metabolites, (+)-salicifoliol and (+)-pinoresinol. Due to the reported biological properties of the lignan natural product

• reaction using N-bromosuccinimide (NBS) in CH2Cl2 at room temperature (1 h), we produced 5 as a single enantiomer (i.e., (+)-5,5'-dibromopinoresinol). Herein, we report the full spectroscopic and spectrometric characterization of this molecule. Furthermore, analogues 6 and 7 are new semisynthetic molecules

• ), which enabled the absolute configuration of 3 to be assigned as 7S,8R,7'S,8'R. Moreover, this is the first report of a crystal structure of (+)-eudesmin (3). In 2015, Lu et al. reported the purification and full characterization of both enantiomers of eudesmin from Acorus tatarinowii, along with the X

Regioselective approach to 5-arylsulfonylisoxazoles and their antimicrobial activity

• Artem S. Sazonov,
• Dmitry A. Vasilenko,
• Denis V. Porfiriev,
• Yuri K. Grishin,
• Rimma A. Gazzaeva,
• Alisa P. Chernyshova,
• Maxim A. Kryakvin,
• Anna A. Baranova,
• Vera A. Alferova and
• Elena B. Averina

Beilstein J. Org. Chem. 2026, 22, 592–602, doi:10.3762/bjoc.22.45

• conditions. MIC (μg/mL) against bacterial and fungal lines. Supporting Information Supporting Information File 8: General synthetic and biological procedures, characterization data and copies of 1H, 13C{1H}, 19F, 31P, 1H-13C HSQC, 1H-13C HMBC NMR spectra, HRMS spectra and the results of the elemental

Molecular tweezer–peptide conjugates disrupt the protein–protein interaction between survivin and histone H3 essential in mitosis

• Catherine Gsell,
• Philipp Rebmann,
• Karina Opara,
• Christine Beuck,
• Peter Bayer,
• David Bier,
• Ingrid R. Vetter and
• Thomas Schrader

Beilstein J. Org. Chem. 2026, 22, 557–567, doi:10.3762/bjoc.22.41

• lyophilization, the product 2a was obtained as fully protonated TFA salt (43%); deprotonation with equimolar aq. NaOH produced the sodium salt of 2a quantitatively. The analytical characterization of 2a turned out to be difficult, because even in DMSO-d6, most NMR signals remained very broad, and in part

Experimental and DFT studies on the regioselective methanolysis of 5-azido-9-oxabicyclo[6.1.0]nonan-4-yl 4-nitrobenzoate isomers

• İlknur Polat,
• Selçuk Eşsiz and
• Emine Salamci

Beilstein J. Org. Chem. 2026, 22, 547–556, doi:10.3762/bjoc.22.40

• regioselective methanolysis of new azido-4-nitrobenzoate epoxycyclooctane isomers and the characterization of the resulting products are described herein. Firstly, treatment of key compound 8-azidocyclooct-4-en-1-ol with 4-nitrobenzoyl chloride followed by an epoxidation reaction and then methanolysis of the

• ring-opening reaction of the epoxides 9 with HCl(g) in MeOH resulted in the formation of chlorohydrin-azidobenzoate isomers 10 and 11 in a total yield of 96% (Scheme 2). Then, for full characterization of the structures of the obtained products, the mixture of chlorohydrins was converted into the

Synthesis and uranyl(VI) extraction performance of a calix[4]pyrrole–tetrahydroxamic acid receptor

• Sara Karnib,
• Rana Baydoun,
• Wissam Zaidan,
• Nancy AlHaddad,
• Omar El Samad,
• Bilal Nsouli,
• Francine Cazier-Dennin and
• Pierre-Edouard Danjou

Beilstein J. Org. Chem. 2026, 22, 486–494, doi:10.3762/bjoc.22.36

• capable of remediating uranium from aqueous environments [38][39]. Results and Discussion PCP HA synthesis and characterization Various strategies have been developed for the synthesis of hydroxamic acid derivatives over the years [40]. Classical and most popular routes involve the direct reaction of

• industrial effluent remediation or for the challenging task of uranium extraction from seawater [79]. Experimental Detailed synthetic procedures, compound characterization (1H and 13C NMR, HRMS), and uranyl extraction protocols, including pH and ligand-to-metal ratio studies, are described in Supporting

Synthesis of a HDAC inhibitor–nanogold probe for cryo-EM visualization in class I HDAC co-repressor complexes

• Wiktoria A. Pytel,
• John W. R. Schwabe and
• James T. Hodgkinson

Beilstein J. Org. Chem. 2026, 22, 480–485, doi:10.3762/bjoc.22.35

• to rt, 18 h, 92%; l) Au–NH2, DMSO, rt, 20 h. Supporting Information Supporting Information File 4: Chemical protocols and characterization data for compounds, biological protocols including cryo-EM grid prep, data collection, and images of micrographs. Acknowledgements We thank Dr. Christos Savva

A facile and practical method for the synthesis of trans-(±)-taxifolin and its derivatives via Darzens reaction

• Bo Peng,
• Panpan Yang,
• Maaz Khan,
• Xiaotong Lin,
• Jiang Wu,
• Peng Fu and
• Qingqing Wu

Beilstein J. Org. Chem. 2026, 22, 443–450, doi:10.3762/bjoc.22.31

• Information File 2: Reaction conditions screening, experimental section with characterization data and copies of spectra. Funding This work was financially supported by the Zhongshan Municipal Natural Science Foundation (Grant# 2023B2019) and the Creative Research Group of Zhongshan City (Lingnan

Synthesis and stereochemical analysis of dynamic planar chiral oxa[7]orthocyclophene

• Yukiho Hashimoto,
• Yuuya Kawasaki,
• Kazunobu Igawa and
• Katsuhiko Tomooka

Beilstein J. Org. Chem. 2026, 22, 436–442, doi:10.3762/bjoc.22.30

• procedures, characterization data, copies of 1H and 13C NMR spectra, and optimized geometries of DFT calculations. Supporting Information File 26: Crystallographic information file of compound 1ac. Acknowledgements We thank K. Imamura (Evaluation center of material properties, IMCE Kyushu University) for

Design, synthesis and biological evaluation of 2,5-diaryloxazolo[4,5-d]pyrimidin-7-ylamines as selective cytotoxic agents against HeLa cells

• Maryna V. Kachaeva,
• Agnieszka B. Olejniczak,
• Marta Denel-Bobrowska,
• Victor V. Zhirnov,
• Yevheniia S. Velihina,
• Stepan G. Pilyo and
• Volodymyr S. Brovarets

Beilstein J. Org. Chem. 2026, 22, 390–398, doi:10.3762/bjoc.22.27

• . Supporting Information Supporting Information File 14: Characterization data and copies of spectra. Acknowledgements We thank Enamine Ltd for the material and technical support. Funding Studies were financed in part by the Ministry of Science and Higher Education within the project POL- OPENSCREEN, the

Dialkylaminoalkylation of β-ketosulfones via ring-opening of 3-sulfonylpyrrolidines

• Evgeny M. Buev,
• Alexander V. Pavlushin,
• Vladimir S. Moshkin and
• Vyacheslav Y. Sosnovskikh

Beilstein J. Org. Chem. 2026, 22, 383–389, doi:10.3762/bjoc.22.26

• optimization of the reaction conditions.a Supporting Information Supporting Information File 12: Experimental section, characterization data and copies of spectra. Funding This work was financially supported by the Russian Science Foundation (Grant 22-73-10008-П).

Spirobarbiturates with a pyrrolizidine moiety: synthesis, structure and biological evaluation

• Arthur A. Puzyrkov,
• Andrew S. Drachuk,
• Ekaterina A. Popova,
• Alexander V. Stepakov and
• Vitali M. Boitsov

Beilstein J. Org. Chem. 2026, 22, 274–288, doi:10.3762/bjoc.22.20

• Information File 38: General information, experimental procedures, characterization data, X-ray data and biological activity data. Acknowledgements This research made use of resources from the Centre for Magnetic Resonance, X-ray Diffraction Centre, Centre for Chemical Analysis and Materials of Saint

A mild and atom-efficient four-component cascade strategy for the construction of biologically relevant 4-hydroxyquinolin-2(1H)-one derivatives

• Dmitrii A. Grishin,
• Kseniia I. Sharkovskaia,
• Ilya G. Kolmakov,
• Daria A. Ipatova,
• Rostislav A. Petrov,
• Nikolai D. Dagaev,
• Dmitry A. Skvortsov,
• Maria G. Khrenova,
• Valeriy V. Andreychev,
• Sergei A. Evteev,
• Yan A. Ivanenkov,
• Roman L. Antipin,
• Olga А. Dontsova and
• Elena K. Beloglazkina

Beilstein J. Org. Chem. 2026, 22, 244–256, doi:10.3762/bjoc.22.18

• pyranoquinoline and in the open-chain ester (see Scheme 6). Supporting Information Supporting Information File 36: Experimental procedures and analytical characterization of all synthesized compounds. Acknowledgements The authors are grateful to Maria E. Filkina for assistance with the design and preparation of

Conformational analysis of difluoromethylornithine: factors influencing its gas-phase and bioactive conformations

• Matheus P. Freitas

Beilstein J. Org. Chem. 2026, 22, 237–243, doi:10.3762/bjoc.22.17

• this work, we present a quantum-chemical study aimed at elucidating the origin of the conformational stability of DFMO. Particular emphasis is placed on natural bond orbital (NBO) analysis [12], which enables a detailed characterization of hyperconjugative interactions and other stereoelectronic

Configuration–packing synergy enabling integrated crystalline-state RTP and amorphous-state TADF

• Ruiyan Wang and
• Yunan Wu

Beilstein J. Org. Chem. 2026, 22, 224–236, doi:10.3762/bjoc.22.16

• activated delayed fluorescence (TADF). Correlating temperature-dependent lifetimes with phase characterization indicate that, in amorphous environments lacking ordered π–π stacking and rigid confinement, the small ΔEST promotes reverse intersystem crossing, yielding delayed fluorescence; whereas in powder