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

• ; Introduction The addition reaction of bromine to diphenylacetylene is one of basic reactions and is recognized as important, because resulting 1,2-dibromo-1,2-diphenylethylene can serve as a precursor for various molecular transformations in organic synthesis [1][2]. This reaction seems to be simple, but some

• -diphenylethylenes (Scheme 1c) [5]. Previous studies reported the selective synthesis of (E)-1,2-dibromo-1,2-diphenylethylene and related compounds, but Br2 or expensive reagent, which was difficult to handle, was often used [6][7][8][9][10][11][12][13][14][15]. Based on these research backgrounds, we have also been

• interested in the selective synthesis of the E isomer of 1,2-dibromo-1,2-diphenylethylene, together with simple purification and separation toward process chemistry, because the compound is an attractive synthetic intermediate for further transformations. During the course of our studies, we have found that

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

• polyacrylate or polystyrene materials. Results and Discussion Synthesis of azobenzene monomers The target azobenzene monomers 1a–f were obtained using a facile three-step synthetic route as shown in Scheme 1. The first step represents an azo-coupling reaction between phenol and the corresponding diazonium

• designed and prepared in a straightforward three-step synthesis. Their fundamental properties were investigated in solution and polymeric matrix. TGA and DSC studies revealed different thermal behavior of mono- and disubstituted derivatives, which most likely results from their (non)planar arrangement as

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

• , inflammation, and myofibroblast activation [18][19][20]. Conversely, intestinal FXR agonism has been demonstrated to promote the release of fibroblast growth factor 19 (FGF19) [21][22], which in turn has been shown to downregulate hepatic bile acid synthesis, lipogenesis, and gluconeogenesis [23][24][25]. A

• MASH. Results and Discussion Chemistry The synthetic routes to the target compounds are outlined in Schemes 4–8. The synthesis of isoxazole intermediate 2 commenced with the condensation of commercially available benzaldehyde I with hydroxylamine to afford oxime intermediate II. Subsequent treatment of

• LiOH or lithium aluminum hydride to obtain compounds Z4–7. The synthesis of compounds Z8–15 followed a similar preparation procedure as for Z1–7. The synthesis of target compounds Z16–29 is illustrated in Scheme 7. Intermediates 8 and 10 were synthesized by the Suzuki cross-coupling reaction using

Preparation of 3-(alkylamino)imidazo[1,2-a]pyridine-2-carbaldehydes via Kornblum oxidation and unexpected ring-opening reactions of the corresponding alcohols under oxidative conditions

• Sandile J. Mkhize,
• Memory Zimuwandeyi,
• Manuel A. Fernandes,
• Amanda L. Rousseau and
• Moira L. Bode

Beilstein J. Org. Chem. 2026, 22, 763–770, doi:10.3762/bjoc.22.58

• Sandile J. Mkhize Memory Zimuwandeyi Manuel A. Fernandes Amanda L. Rousseau Moira L. Bode Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Private Bag 3, PO WITS, 2050, South Africa 10.3762/bjoc.22.58 Abstract The first synthesis of 3-(alkylamino)imidazo[1,2-a

• ester. In this paper, we describe the synthesis of a library of derivatives of 8, whose imidazo[1,2-a]pyridine core could be accessed via the Groebke–Blackburn–Bienayme (GBB) multicomponent coupling reaction [20][21][22][23]. Results and Discussion In order to access our initial target compounds 7, the

• to obtain the desired aldehydes led to a modification of the planned synthesis. A decision was made to convert alcohols 17 into the corresponding tosylate derivatives 19 (Scheme 6) and then react these with anilines to obtain the desired products 8. To our complete surprise, reaction of 17b and 17d

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

• , MEDING. Laboratorio de Biología molecular. Escuela de Medicina, Universidad de Valparaíso, Chile Instituto de Ciencias Aplicadas, Facultad de Ingeniería, Universidad Autónoma de Chile, Av. del Valle Sur 534, Santiago 8580640, Chile 10.3762/bjoc.22.57 Abstract The synthesis and structural

• be possible to evaluate the contribution of different functions attached to ring A. Thus, herein the synthesis of analogs 17–22, starting from the precursor 16, is described. All compounds have been fully characterized by spectroscopic techniques (IR, 1D, 2D NMR and HRMS). The biological activities

• The synthesis of new BR analogs 17–22 (Figure 2) and compounds 23–28 has been carried out using the olefinic precursor 16 according to previously described procedures (Scheme 1) [28][29]. Treatment of olefine 16 with p-R-PhCOCl in DMAP/py/CH2Cl2, leads to compounds 23–28 with high yields (78.0–96.7

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

• experimental and computational study of the diastereoselectivity of cyclic sulfone synthesis by reaction of Rongalite with doubly electrophilic dienones is presented. Computational methods, including density functional theory, conformational search methods, and internal reaction coordinate methods, have been

• molecules are desirable, particularly in the light of the general need for more sustainable chemical synthesis. Recently, there has been significant progress in the use of SO2 equivalents and bulk inorganic high oxidation state sulfur compounds for the direct incorporation of sulfones [2][3]. Despite these

• used as a bleaching agent in the dyeing industry for more than a century [5][6]. Over the last 10 years particularly, it has begun to join the toolbox of reagents in organic synthesis, and shows diverse reactivity. It has been employed in reductions, radical processes and as a reagent for C1 transfer

Synthesis of heterocycles based on azomethine ylides from α-amino acids (or amines) and carbonyl compounds

• Ekaterina V. Berezhnaya,
• Alexander I. Ponyaev,
• Vitali M. Boitsov and
• Alexander V. Stepakov

Beilstein J. Org. Chem. 2026, 22, 705–741, doi:10.3762/bjoc.22.55

• compounds; catalysis; (3 + 2) cycloaddition; decarboxylation; dipolarophiles; iminoesters; polycyclic compounds; spirocyclic compounds; stereoselectivity; Introduction The 1,3-dipolar cycloaddition is one of the most popular pericyclic reactions in organic synthesis, in which a dipole molecule interacts

• ]. The use of azomethine ylides as dipoles is necessary for the synthesis of pyrrolidine systems, which are often found in natural products and are important structural fragments of pharmaceuticals [5]. This method is also used to obtain pyrrolizidine derivatives, which are the structural basis of

• strategy is that the synthesis is often carried out under mild conditions without the use of a catalyst, and despite this, the resulting cycloadducts exhibit pronounced regio- and stereoselectivity [9][10][11]. In the second case, the generation of azomethine ylides from iminoesters is often realized using

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

• purity (>95%). Semisynthetic analogues 3−5 are known compounds [25][26]. However, some of these compounds have not been fully characterized. Regarding compound 5, this molecule had previously been reported as an intermediate in the total synthesis of racemic pinoresinol [25]. Through a bromination

• collected on a Rigaku XtaLAB synergy diffractometer using Cu Kα radiation at 100.0(1) K using an Oxford Cryostream cooling device. The structure was solved by direct methods and difference Fourier synthesis [36]. Hydrogen atoms bound to the carbon atom were placed at their idealized positions and included

Synthesis of depressin, cryptomeridiol and 4-epi-cryptomeridiol enabled by a terpenoid chiral pool-producing platform

• Yao Kong,
• Tao Wang,
• Chen Wang,
• Pengcheng Zhang,
• Yuanning Liu,
• Kaibiao Wang,
• Fen Liu,
• Hongli Jia and
• Zhengren Xu

Beilstein J. Org. Chem. 2026, 22, 683–690, doi:10.3762/bjoc.22.53

• skeleton and a C5-keto group. Key strategies for the synthesis of depressin, as well as its casbene skeleton reported so far focused on the formation of the challenging 14-membered ring system. Cryptomeridiol (2) and 4-epi-cryptomeridiol (3) are two eudesmane-type sesquiterpene diols produced by a variety

• of different plants with broad biological activity. Most of the syntheses focused on the transformation of chiral pool substrates into their trans-6/6-fused ring system. We herein report the synthesis of compounds 1–3 by taking advantage of an expanded chiral pool strategy, in which the terpenoid

• hydroxy group allowed the synthesis of compound 1 from 4 in nine steps. Selective acid-mediated 5,10-transannular cyclization of 5 followed by hydration reaction furnished both products 2 and 3 in two steps. Keywords: chemoenzymatic synthesis; chiral pool; isopentenol utilization pathway; terpene

Harnessing light energy with molecules

• Grace G. D. Han,
• Mogens Brøndsted Nielsen and
• Hermann A. Wegner

Beilstein J. Org. Chem. 2026, 22, 680–682, doi:10.3762/bjoc.22.52

• article by Wahl and co-workers [21], ring-opening of photogenerated azetidinols was used as a strategy for the convenient synthesis of aminodioxolanes. Photochemical denitrogenation reactions of bicyclic azoalkanes present a way to prepare strained bicyclic compounds. Further, Gomes and Lopez [22] report

Using generative AI to transform peptide hits into small molecule leads

• Joshua Mills and
• Yu Heng Lau

Beilstein J. Org. Chem. 2026, 22, 672–679, doi:10.3762/bjoc.22.51

• triaging generated candidates prior to more resource-intensive modelling, laboratory synthesis, and evaluation in functional assays. Deep learning for protein structure prediction The growing wealth of structural data in the Protein Data Bank, along with ongoing improvements in computational processing

Photoorganocatalytic trifluoromethylation of (het)arenes in green conditions

• Egor N. Boronin,
• Svetlana E. Kaurkina,
• Milena M. Svetlakova,
• Anton S. Bolshakov,
• Maxim V. Arsenyev,
• Vasilii F. Otvagin,
• Alexey Yu. Fedorov,
• Timothy Noël and
• Alexander V. Nyuchev

Beilstein J. Org. Chem. 2026, 22, 662–671, doi:10.3762/bjoc.22.50

• amenable to scale-up, with continuous-flow operation delivering a significant increase in space–time yield, highlighting its potential for sustainable synthesis of CF3-containing molecules. Keywords: green chemistry; photocatalysis; photochemistry; trifluoromethylation; Introduction Trifluoromethylated

• , atom-economical, and cost-effective photocatalytic protocol for the trifluoromethylation of arenes and heteroarenes in a green solvent (Scheme 1e). The cost of reagents is one of the key factors in large-scale synthesis. We have updated the price comparison table of trifluoromethylating agents

• indicate that among the solvents employed in the procedures shown in Scheme 1, ethyl acetate represents a more environmentally sustainable alternative. Herein, as a continuation of our studies on photochemical approaches to the synthesis of fluorine-containing compounds [23][24][25] and on the development

Towards the targeted protein degradation of CK2: design and synthesis of CAM4066-based PROTACs

• Sophie Day-Riley,
• Sona Krajcovicova,
• Aryaman Raj Sokhal,
• Jan L. Venne,
• Paul Brear,
• Marko Hyvönen,
• Benjamin C. Whitehurst,
• Jason S. Carroll and
• David R. Spring

Beilstein J. Org. Chem. 2026, 22, 611–619, doi:10.3762/bjoc.22.47

• potent and selective PROTAC targeting CK2 might be valuable in the evaluation of specific degradation of CK2 as a therapeutic approach. Herein, we report the design and synthesis of a series of CK2-targeting PROTACs. CAM4066 was selected as the warhead to enable CK2-specific target engagement. We

• construction. The synthesis of the ATP-site binder began with the alkylation of commercially available methyl 3-aminobenzoate (3) using bromoacetyl bromide. Although initial purification via silica gel chromatography led to substantial product loss, isolation by simple aqueous workup afforded the intermediate

• synthesis see Supporting Information File 1, section 1.3). In parallel, PEG-based linkers bearing terminal alkyne handles were synthesised for modular CuAAC-based PROTAC assembly. The αD binder 16 had been synthesised via a two-step reaction. First, the phenolic group of 15 was converted into the

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

• Bioengineering and Bioinformatics, Lomonosov Moscow State University, 119991 Moscow, Russian Federation 10.3762/bjoc.22.45 Abstract This study presents a novel regioselective synthesis of 3-electron-withdrawing-group-(EWG)-substituted 5-sulfonyl- and 5-sulfinylisoxazoles from 3-EWG-5-nitroisoxazoles via

• studies indicate that these compounds induce the bacterial SOS response without inhibiting DNA synthesis-related enzymes such as DNA polymerase I, DNA gyrase, or topoisomerases I and IV, suggesting activation via bacterial reductases. These findings highlight the potential of these isoxazole derivatives

• as promising antimicrobial agents and provide new insights into their mechanism of action. Keywords: antimicrobial activity; aromatic nucleophilic substitution; isoxazoles; oxidation; sulfonylisoxazoles; Introduction The isoxazole ring represents an important building block for the synthesis of

Design and synthesis of an erdafitinib-based selective FGFR2 degrader

• Yumeng Jin,
• Shidong Wang,
• Sihan Pan,
• Shuqi Huang,
• Weichen Zhou,
• Xiaohao Huang,
• Lei Zheng and
• Lingfeng Chen

Beilstein J. Org. Chem. 2026, 22, 583–591, doi:10.3762/bjoc.22.44

• . Synthesis of PROTACs towards FGFR2. Reagents and conditions: (a) K2CO3, Pd (dppf)Cl2, 1,4-dioxane/H2O 4:1, 100 °C, 5 h; (b) 3,5-dimethoxyaniline, Pd2(dba)3, BINAP, Cs2CO3, toluene, 100 °C, 12 h; (c) (2-bromoethoxy)-tert-butyldimethylsilane, NaH, DMF, rt, 12 h; (d) tetrabutylammonium fluoride, THF rt, 12 h

Continuous-flow carbonyl hydrogenation under subatmospheric to atmospheric hydrogen pressure enabled by robust heterogeneous Pt–Fe catalysts

• Hiroyuki Miyamura,
• Ryosuke Kajiyama,
• Shun-ya Onozawa,
• Yoshihiro Kon and
• Shū Kobayashi

Beilstein J. Org. Chem. 2026, 22, 575–582, doi:10.3762/bjoc.22.43

• , including ketones and aldehydes, to alcohols is a fundamental and important reaction in organic synthesis. One of the most ideal methods is catalytic hydrogenation, however, the hydrogenation of ketones generally requires harsh reaction conditions, such as high temperature and high pressure. We developed a

• : bimetallic nanostructure; carbonyl reduction; continuous-flow reaction; heterogeneous catalyst; subatmospheric hydrogen; Introduction The reduction of carbonyl compounds, ketones and aldehydes to alcohols is a fundamental and important reaction in organic synthesis that can provide valuable chemicals such

• ]. Recently, continuous-flow organic synthesis has attracted much attention from both academia and industry, because it offers numerous advantages, such as not only a high productivity with limited space but also realizing green sustainable syntheses minimizing required energy and resources. When

Kinetic resolution of racemic planar-chiral vinylcymantrenes by molybdenum-catalyzed asymmetric metathesis dimerization

• Haruna Imazu,
• Hitoshi Izu,
• Yasuhiro Ohki and
• Masamichi Ogasawara

Beilstein J. Org. Chem. 2026, 22, 568–574, doi:10.3762/bjoc.22.42

• resolution; molybdenum; olefin metathesis; planar chirality; Introduction The development of the well-defined molybdenum- [1][2] or ruthenium-alkylidene [3][4][5] catalysts has proven the olefin metathesis reaction to be a powerful tool in organic synthesis. Asymmetric extension is a recent trend in

• the excellent tolerance of the Mo-/Ru-metathesis catalysts toward the organometallic substrates. The olefin metathesis protocols could be extended to the asymmetric synthesis of diverse planar-chiral transition metal complexes either by the kinetic resolution of the racemic substrates [14][15][16] or

• demonstrated to be excellent chiral scaffolds in asymmetric synthesis, however, enantioselective synthesis of such planar-chiral complexes is still relatively undeveloped and remains as a challenging problem in asymmetric synthesis [24][25][26][27][28][29]. A new type of asymmetric olefin metathesis reaction

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

• approximately 8-fold gain in affinity by attaching the tweezer moiety to the peptide, provided that the tweezer could reach a suitable binding partner as well. To allow a general commercial synthesis of the phosphorylated H3-peptide sequences for the tweezers, we used an azidoornithine extension at the C

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

• process, highlighting its precision and efficiency. Keywords: azides; 8-azidocyclooct-4-en-1-yl 4-nitrobenzoate; DFT; epoxycyclooctane azide; methanolysis; Introduction Organic azides are very important precursors for the preparation and synthesis of various nitrogen-containing compounds, as well as

• methodologies for the preparation of this class of compounds are of considerable interest. Azides have traditionally been used as protected primary amine equivalents. Therefore, in our previous studies, we employed azides containing eight-membered rings as precursors in the synthesis of C8-aminocyclitols [12

• ][13][14][15][16][17][18][19]. The ring-opening reactions of bicyclic epoxides are of significant importance and scientific interest due to their high ring strain, their strategic role in the construction of complex molecular architectures, and their utility in the synthesis of natural products

Melifoliox B, a novel phloroglucin derivative isolated from Melicope barbigera (Rutaceae) and synthesis of new oxidation products from melifoliones A and B

• Horst Weber,
• Kim-Thao Tran-Cong,
• Bernhard Mayer,
• Guido J. Reiss,
• Iryna S. Konovalova,
• Marc S. Appelhans,
• Kenneth R. Wood and
• Claus M. Passreiter

Beilstein J. Org. Chem. 2026, 22, 535–546, doi:10.3762/bjoc.22.39

• synthesis of 4 and its possible isomer 3, the required compounds 1 and 2 were synthesized as a mixture of the isomers starting from chromene 5, briefly heated in a closed microwave apparatus with catalytic amounts of acetic acid. Forced heating of 5 in acetic acid or use of stronger acids lead to the

• diacetate (EDDA). However, synthesis of 2 was difficult. Despite numerous attempts, we only were able to get mixtures of both melifoliones with minor amounts of 2. Since all attempts to separate both isomers on a preparative scale failed, we were only able to record NMR spectra from a very small quantity of

• -position in regard to the OH-group at C-10b (Table 2). Synthesis of melifoliones Melifolione A (1) was prepared according to the method of Wang and Lee [5] by heating phloroacetophenone and citral with ethylene-diammonium diacetate (EDDA) in DMF. However, reaction of the educts in pyridine at 60 °C led to

Get a better glimpse on sequential photoreactions of trisnorbornadienes with ¹⁹F NMR spectroscopy

• Julian Felix Maria Hebborn,
• Ben Eric Merten,
• Thomas Paululat and
• Heiko Ihmels

Beilstein J. Org. Chem. 2026, 22, 527–534, doi:10.3762/bjoc.22.38

• comparison of the synthesis and photophysical properties of the fluoro-substituted norbornadiene 1f with the ones of the parent compound 1b revealed that the yield of the Suzuki–Miyaura coupling reaction is significantly lower for the former [22], presumably because of the steric hindrance induced by the

• 19F NMR spectroscopy, further structural optimization is necessary for application purposes. Experimental Synthesis 1,3,5-Tris(bicyclo[2.2.1]hepta-2,5-dien-2-yl)-2,4,6-trifluorobenzene (1f) A mixture of 1,3,5-tribromo-2,4,6-trifluorobenzene (212 mg, 575 µmol), 4,4,5,5-tetramethyl-2-(bicyclo[2.2.1

• cycloreversion of 2a. Synthesis and photochromic reaction of trisnorbornadiene 1f to the trisquadricyclane 2f0,3 (numbering of quadricyclanes 2fm,n: m = number of norbornadiene units, n = number of quadricyclane units). Stepwise photoreaction of 1f to 2f0,3 (numbering of quadricyclanes 2fm,n: m = number of

Modern synthetic pathways towards eribulin and its subunits

• Sebastian Dominik Graf

Beilstein J. Org. Chem. 2026, 22, 495–526, doi:10.3762/bjoc.22.37

• approaches is rigorously ongoing. Recent procedures mainly focus on more efficient and scalable techniques for the assembly of the 4 key fragments of eribulin. But also new pathways for the total synthesis have emerged in the last decade. In this review the latest advancements towards the construction of

• eribulin are summarized. Keywords: breast cancer; drug manufacturing; eribulin; Halaven; total synthesis; Introduction Eribulin (1) is a truncated derivative of halichondrin B (2), a complex natural product originally isolated from the marine sponge Halichondria okadai (Figure 1) [1][2][3][4][5]. Already

• described the total synthesis of the marine natural product [19] and shortly thereafter, also its simplified structure, 1, was assembled and showed similar anticancer behavior [19][21]. Since 2010, the mesylate salt of 1 is approved by the U.S. Food and Drug Administration (FDA) for the treatment of

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

• extractants. Here, we report the design and synthesis of PCP HA, a phenoxycalix[4]pyrrole scaffold functionalized with four hydroxamic acid (HA) groups, and evaluate its uranium(VI) extraction potential. PCP HA was synthesized from its ester precursor (PCP E) via hydroxyaminolysis using KOH, achieving a 95

• 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

• aldehydes [45], alcohols [46], and amides [47] have also been reported. However, the literature states that there is no particular reagent or reaction condition that can serve as a general rule for the synthesis of hydroxamic acids [48]. In this study, the direct reaction of hydroxylamine with the PCP ester

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

• LE1 7RH, UK 10.3762/bjoc.22.35 Abstract Class I histone deacetylases (HDACs 1–3) serve as catalytic subunits within seven multiprotein co-repressor complexes, each of which has distinct functions in the cell. We report the synthesis of a HDAC inhibitor–nanogold probe, derived from the class I HDAC

• synthesize a nanogold-conjugated HDAC inhibitor and evaluate its applicability in single-particle cryo-EM to unambiguously determine the positioning and orientation of the HDAC active site within the CoREST complex. Results and Discussion Design and synthesis of a HDAC inhibitor–nanogold probe For the basis

• routes (Scheme 1) [14][15][18]. Intermediates 5–7 were prepared in a manner analogous to Smalley et al. [14]. The first step in the linker synthesis for Au–(CI-994) involved a monoprotection of nonanedioic acid with a benzyl group to give 5 which proceeded in moderate yield due to the formation of the

Recent advances in the stereoselective synthesis of distal biaxially chiral molecules

• Fanxing Zhou,
• Chen Zhang,
• Lingyu Sun,
• Yiyun Fang,
• Siming Zheng,
• Lina Hu,
• Mengyang Shen,
• Zhen Zhao,
• Wei Xu,
• Yunqiang Sun and
• Zi-Qiang Rong

Beilstein J. Org. Chem. 2026, 22, 461–479, doi:10.3762/bjoc.22.34

• distal axial chiralities are widely applied in chiral ligands, natural products, and anticancer agents, with their unique spatial configurations endowing them with distinctive functions and values. Although significant progress has been made in the asymmetric synthesis of distal biaxial chirality

• biaxial chirality, multistep sequential generation, and conversion from central to biaxial chirality, with the aim of providing new perspectives and methodologies for further development in this area. Keywords: axially chiral compounds; stereoselective synthesis; Introduction In recent years, axially

• "-ternaphthalene compounds [35]. This work significantly advanced the development of bi- and multiaxial chirality. The synthesis of multiaxial chiral molecules requires appropriate steric hindrance to elevate the rotational energy barrier of each chiral axis [36], and the spatial interactions between axes are