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

• Tanacetum parthenium) [52] encoding genes were synthesized and cloned into the pET28a-based plasmid, to give pET28a-cs and pET28a-gas, respectively. The E. coli heterologous host was then co-transformed with pXT02007/pET28a-gas and pXT02013/pET28a-cs, to afford strains XT02019 (for production of germacrene

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

• approaches of optimization with regard to their light harnessing efficiency, energy storage capacity, and storage time. Structural modifications and studies of the norbornadiene/quadricyclane (NBD/QC) photo-/thermoswitch couple are covered in several articles. In a publication by Kerzig, Ihmels, and co

• -workers [4], the π-system of monoaryl-substituted NBDs was synthetically extended by acetylenic bridges. In addition, Hebborn, Ihmels, and co-workers [5] show that 19F NMR spectroscopy enables unambiguous identification of mono- and bisQC intermediates in the sequential photoreactions of a fluorinated

• structure by a heteroatom (oxygen or nitrogen) in donor–acceptor, push–pull NBD derivatives are reported. In a computational study, Pawar and co-workers [7] further expanded the NBD structure by elongating the unsaturated bridge with different heteroatoms or functional groups. Azobenzenes, interconverting

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

• functionality to recapitulate the pharmacophore of the original peptide (Class D according to the classification proposed by Grossmann and co-workers [10]). The challenge of transforming a peptide binder into a small molecule mimic is not new [11]. Indeed, there are well-known historical examples of blockbuster

• experimental co-crystal structure of the bound complex, standard medicinal chemistry principles are used to probe structure–activity relationships (SAR) and determine the key interactions that form a minimal pharmacophore, supported by classical physics-based molecular modelling methods such as molecular

• dynamics (MD) and docking (Figure 1). As an illustrative example, Yoshida and co-workers at Shionogi reported the design of small molecule inhibitors of nicotinamide N-methyltransferase [14] and β-herpesvirus proteases [15], starting from cyclic peptide hits obtained by mRNA display with flexible in vitro

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

• approaches can be regarded as among the most environmentally sustainable methods for trifluoromethylation. MacMillan and co-workers reported the photochemical trifluoromethylation of arenes and heteroarenes using Ru- and Ir-based photocatalysts together with trifluoromethanesulfonyl chloride (TfCl) in the

• transformations were performed in acetonitrile, which reduces their ecological compatibility, particularly for large-scale applications. Tlili and co-workers have described the use of an organic photocatalyst for the CF3-functionalization of styrenes with the Langlois reagent (sodium trifluoromethanesulfinate

Advantages of PROTACs in achieving selective degradation of homologous protein families

• Luxi Yang,
• Xinfei Mao,
• Jingyi Zhang,
• Jing Shu,
• Wenhai Huang,
• Xiaowu Dong,
• Yinqiao Chen and
• Mingfei Wu

Beilstein J. Org. Chem. 2026, 22, 628–661, doi:10.3762/bjoc.22.49

• pharmaceutical chemists. In 2019, Gray, Zhang and co-workers designed a PROTAC-1 (1) to degrade CDK4/6 [21]. To construct compound 1 they used the CDK4/6 inhibitor palbociclib as the POI ligand, pomalidomide, which combines with CRBN as the E3 ligand and a 4-carbon alkyl linker to connect them. The compound can

• ability to target the degradation of CDK6, and proteomics results also show that compound 2 has no degradation effect on CDK4. In 2020, Benowitz and co-workers carried out a project to explore the impact of different E3 ligands on the selective degradation of CDK4/6 [57]. In their research, they designed

• ligand and E3 ligand. Similarly, the research results show that compound 3 can also selectively degrade CDK6. Meanwhile, Rana, Natarajan and co-workers developed a PROTAC-6 (4) based on palbociclib and pomalidomide [58] (Figure 2). In the study, the researchers evaluated the degradation effect of

Hydrogen production from formic acid catalyzed by NHC–Cu complexes

• Orlando Santoro and
• Catherine S. J. Cazin

Beilstein J. Org. Chem. 2026, 22, 620–627, doi:10.3762/bjoc.22.48

• have also been explored. Beller and co-workers reported the first Fe catalyst bearing a phosphine ligand able to produce H2 with a TON of 1942 in the absence of additives [32]. A well-defined pincer–Fe complex allowing FA decomposition was reported by Milstein and co-workers [33]. While high TONs (up

• such as Co [35][36], Ni [37][38], Al [39][40], and Mn [41][42][43] have been released. In this scenario, copper systems remain widely unexplored and, generally, have displayed low activity, regardless of the oxidation state of the Cu precursor and of the presence/absence of additives [44][45][46][47

• ]. Finally, a Cu(I)–formato complex able to promote FA dehydrogenation in the absence of any additive was very recently reported by Berthet, Cantat and co-workers [48]. During the past decades, NHC–Cu complexes have shown to be efficient catalysts in a plethora of reactions. Indeed, they guarantee better

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

• broader kinome perturbation. The first design objective was therefore to identify a suitable exit vector for linker attachment that would allow productive E3-ligase recruitment without compromising the established binding geometry of CAM4066. Inspection of the co-crystal structure of 1 bound to CK2α

• yield acid S13. Isothermal titration calorimetry (ITC) revealed that S13 bound CK2α with a dissociation constant (Kd = 600 nM) comparable to that of CAM4066 (350 nM; Figure 1C). This indicated that the exit vector modification and linker installation were well tolerated. Co-crystallisation of S13 with

• suitable for linker installation, and introduction of a secondary amine at this position provided a versatile handle for downstream functionalisation. The resulting CAM4066-derived ligand–linker analogue S13 retained high-affinity binding to CK2α and preserved the characteristic bivalent binding mode in co

Computational prediction of C–H hydricities and their use in predicting the regioselectivity of electron-rich C–H functionalisation reactions

• Rasmus M. Borup,
• Nicolai Ree and
• Jan H. Jensen

Beilstein J. Org. Chem. 2026, 22, 603–610, doi:10.3762/bjoc.22.46

• electron-rich C–H functionalisation reactions. Methods Datasets To validate our QM workflow, we use a dataset of 35 experimental C–H hydricities in dimethyl sulfoxide (DMSO, 26 compounds) and acetonitrile (MeCN, 9 compounds) from Parker and co-workers [7]. As 35 C–H hydricities are insufficient to train an

• hydricities and BDEs. Using the ALFABET model developed by Paton and co-workers to predict BDEs [4][5][37], we find that our QM-computed hydricities exhibit a better correlation with experimental data compared to BDEs, with an MAE of 7.58 kcal/mol and an RMSE of 9.44 kcal/mol, see Figure 3. Refer to section 3

• nine reactions highlighted by Cernak et al. [6] and add an additional reaction (compound 6, see below). For each reactant, we compute the hydricities as well as the BDEs using the ML method developed by Paton and co-workers [4][5] and the percentage of buried volume of the relevant C atoms (%Vbur

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

• purpose the clinically validated inhibitor erdafitinib as a POI binder that selectively targets FGFR2. Based on the analysis of the co-crystal structure of erdafitinib bound to the FGFR kinase domain (PDB: 5EW8, https://doi.org/10.2210/pdb5EW8/pdb) [30], we observed that the aliphatic amine group is

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

• easily oxidize to Fe(II) during the filtration and heating processes, resulting in the formation of a bimetallic structure comprising Pt(0) and Fe(II). Pt‒Au, Pt‒Co, and Pt‒Ni bimetallic catalysts immobilized on DMPSi‒Al2O3 were also prepared by the same procedure. Comparison of the catalysts in the

• , Pt‒Co and Pt‒Fe bimetallic catalysts immobilized on DMPSi‒Al2O3 showed high activity with minimal by-product formation (Table 1, entries 7‒11). Especially, Pt‒Fe/DMPSi‒Al2O3 (Fe/Pt = 0.62‒2.3) demonstrated excellent catalytic performance under the continuous-flow conditions giving the desired product

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

• interaction by roughly one order of magnitude (from 1 µM to 120 nM Kd). For further structural proof we attempted co-crystallization of survivin with our new tweezer H3 conjugate. Unfortunately, crystallization of full length survivin 1–142 was difficult to reproduce and often resulted in low-quality crystals

• the included side chain protons [12][13]. HPLC–HRMS analysis finally produced a single chromatographic signal with clean molecular ion peaks for [M + 2H]2+ and [M + 3H]3+. The high purity of 2a was further demonstrated by successful co-crystallization of this tweezer peptide conjugate with survivin

• limiting the crystallization conditions [22]. Other co-crystallized peptides are AKERC from the N-terminus of shugoshin1 (6.2 µM, PDB ID 4A0I) [8] and a Smac-DIABLO 15-mer-peptide with only 121 µM affinity, that still crystallized at sufficiently high concentrations in complex with survivin (PDB ID 3UIH

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

• pathway. The conformational preferences of the cyclooctane ring were analyzed based on the eight consecutive dihedral angles (τ1–τ8, °), which are summarized in Table 2, following the classification proposed by Pakes and co-workers [24]. TS1 displays a predominantly boat-chair geometry, with only one over

• -twisted dihedral angle (τ3 = 94°), indicating a moderately distorted boat-chair conformation. In contrast, TS2 exhibits a characteristic twist-boat-chair arrangement, evidenced by the co-existence of a strongly over-twisted segment (τ2 = 101.8°) and a nearly planar dihedral (τ6 = 4.0°). A similar trend is

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

• within their isolation study on halichondrin B, in 1986, Hirata and Uemura showed its promising activity against murine cancer cells [6], which led to a great interest in the pharmaceutical society [7][8][9][10][11][12][13][14][15][16][17][18][19][20]. Only 6 years later, Kishi and co-workers first

• ][71]. In 2016, Bauer already reported on the current state of research, focusing on contributions from Kishi and co-workers and the Eisai process [71]. However, due to the great demand of 1, this research field continues to grow. In this context, the following review should summarize and explain

• modern approaches towards the key fragments and total synthetic strategies for 1 in recent years. Review In 2016, Konda and co-workers reported two approaches for the assembly of the tetrasubstituted tetrahydrofuran unit of 1 (Scheme 2 and Scheme 3) [72]. For the first path, (S,S)-tartaric acid (13) was

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

• inhibitor CI-994, for cryo-electron microscopy (cryo-EM) visualization of the HDAC catalytic domain within class I HDAC co-repressor complexes. The nanogold probe retained HDAC inhibitory activity comparable to CI-994 against the HDAC1-LSD1-CoREST complex in vitro. In cryo-EM studies, 2D class averages

• domain within the CoREST complex. Keywords: CI-994; co-repressor complex; CoREST; cryo-EM; gold nanoparticle; HDAC; Introduction Histone deacetylase (HDAC) enzymes catalyze the hydrolysis of acetyl groups from N-acetylated lysine residues in histone proteins. HDACs are also capable of the deacetylation

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

• demonstrated that such one-step catalytic approaches not only streamline the synthesis of structurally complex biaxial molecules but also open new avenues for their applications in catalysis, drug discovery, and functional materials. In 2004, Shibata and co-workers reported a novel iridium-catalyzed asymmetric

• [41]. This strategy delivered excellent enantioselectivity, diastereoselectivity, and overall efficiency, underscoring its unique advantages in the synthesis of multiaxially chiral scaffolds. In parallel, Tanaka and co-workers advanced a [2 + 2 + 2] cycloaddition strategy to realize an asymmetric

• studies have further broadened the synthetic toolbox for remote biaxial chirality. Du and co-workers designed a series of chiral phosphoric acid catalysts derived from protected axially chiral diols 13, employing a boronic acid-mediated coupling strategy to construct remote biaxially chiral phosphoric

Concept-driven strategies in target-oriented synthesis

• David Yu-Kai Chen,
• Chao Li and
• Yefeng Tang

Beilstein J. Org. Chem. 2026, 22, 451–454, doi:10.3762/bjoc.22.32

• , Xuefeng Jiang and co-worker), convergent synthesis (khayanolide limonoids, Li Zhang, Peirong Rao et al.), stereodivergent synthesis (aspera chaetominines, Pei-Qiang Huang et al.), 1,3-diol desymmetrization (review, Zhifeng Shi, Zhiquiang Ma et al.), 1,3-dicarbonyl reductive desymmetrization (review, Fu

• -She Han and co-worker), bioinspired synthesis (review, Huilin Li, Xuegong She et al.), biosynthesis (fusicoccane diterpenoids, Yonghui Zhang, Ying Ye, Zheng Xiang et al.), chemoenzymatic synthesis (rhodexin A, Qianghui Zhou et al.)]; (ii) comparative analysis of target-oriented synthesis [complanadine

• A (review, Mingji Dai and co-worker), ryania diterpenoids (review, Jin-Bao Qiao, Yu-Ming Zhao and co-worker), illisimonin A (review, Ming Yang and co-worker)]; and (iii) methodology towards target-oriented synthesis [oxidative dearomatization (simonsol C, Hong-Bo Qin et al.), reductive

Synthesis and anti-cancer activity of naphthalimide–organylselanyl conjugates

• Rajkumar Ravi and
• Selvakumar Karuthapandi

Beilstein J. Org. Chem. 2026, 22, 416–435, doi:10.3762/bjoc.22.29

• cancer cell line. Molecular docking simulation revealed strong binding interaction and affinities towards the tyrosine kinase domain of epidermal growth factor receptor (EGFR), and the protein–ligand interaction resembles the interaction found in the co-crystallised protein–erlotinib complex. Result and

• conformation (4HJO). The docking results revealed that both ligands fit well within the binding pocket of the EGFR tyrosine kinase domain. The binding interactions were further validated by comparison with the crystal structures of the active (1M17) and inactive (4HJO) forms of EGFR complexed with the co

• carbonyl oxygen surface promotes hydrogen-bond formation. The binding site interactions of compounds 7 and 8 with the tyrosine kinase were further validated by comparison with the crystal structure of 1M17 with co-crystallised ligand erlotinib (Figure 9c), showing that both compounds form similar active

Cone p-aminocalix[4]arenes enriched with ‘clickable’ alkyne or azide functionalities

• Ilia Korniltsev,
• Vasily Bazhenov,
• Alexander Gorbunov,
• Dmitry Cheshkov,
• Stanislav Bezzubov,
• Vladimir Kovalev and
• Ivan Vatsouro

Beilstein J. Org. Chem. 2026, 22, 399–415, doi:10.3762/bjoc.22.28

• calixarene tetraaryl- and tetraarylsulfonylureas if co-dissolved in a 1:1 molar ratio [51][52][53]. Furthermore, tetraureas 47–51 contain relatively bulky substituents at the phenolic oxygen atoms, which may influence the conformational behavior of the macrocycle (e.g., pinched cone-to-pinched cone

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

• , sarcosine, and paraformaldehyde in PhMe/MTBE, followed by treatment of the reaction mixture with an alkyl halide, and subsequent heating of the precipitated quaternary ammonium salt in the presence of Cs₂CO₃ and a nucleophile – we proceeded to apply this methodology to other β-ketosulfones. Next, we

• -amine (5) in 77% yield (Scheme 4). This observation prompted us to examine methoxy and morpholine adducts 4a and 4o in the same process that resulted in the isolation of sulfonylamine 5 in 69 and 48%, respectively. The literature search revealed that previously Langler and co-authors observed the

Electrosynthetic access to unsymmetrical oxaza[8]helicenes with high chiral stability and strong circularly polarized luminescence (CPL)

• Tin Zar Aye,
• Rubal Sharma,
• Muthu Karuppasamy,
• Daiya Suzuki,
• Haruka Nakajima,
• Yoshitane Imai,
• Mitsuhiro Arisawa,
• Mohamed S. H. Salem and
• Shinobu Takizawa

Beilstein J. Org. Chem. 2026, 22, 372–382, doi:10.3762/bjoc.22.25

• comparatively underdeveloped [30], despite the appealing prospect of higher barriers to enantiomerization and richer optoelectronic behavior [31]. In 2021, Yorimitsu and co-workers disclosed a series of symmetric dihetero[8]helicenes I–IV that exhibited intriguing chiroptical properties utilizing the

• characteristic transformations of the organosulfur functionality [32][33]. In 2024, Badani, Karnik, and co-workers accessed one member of this class, 7,12-dioxa[8]helicene I, through a sequence featuring photochemical E–Z isomerization, electrocyclization, and oxidative aromatization [34]. In parallel, Liu and

• co-workers introduced the π-extended azabora[8]helicene V with exceptional chiroptical signals and high brightness, emphasizing the promise of this class of chiral molecules (Scheme 1A) [35]. Despite these advances, unsymmetrical hetero[8]helicenes – where heteroatoms occupy non-equivalent positions

Ring contraction and ring expansion reactions in terpenoid biosynthesis and their application to total synthesis

• Nicolas Kratena,
• Nicolas Heinzig and
• Peter Gärtner

Beilstein J. Org. Chem. 2026, 22, 289–343, doi:10.3762/bjoc.22.21

• , thousands of closely related compounds could be identified. Among these, the more structurally interesting, rearranged or highly oxidised members can often only be vaguely traced back to their biogenetic origin based on co-isolation and biochemical intuition. Synthetic approaches can sometimes help to solve

• elucidated by Dickschat and co-workers in 2023, describing the biosynthesis of the spirocyclic diterpene spiroluchuene A (20, see Scheme 5), catalysed by the synthase AlTS (Aspergillus luchuensis terpene synthase) [70]. Geranylgeranyl diphosphate (GGPP, 12) is initially cyclised through the well-known 1,10

• carbocation 29d, according to the mechanistic proposal by Coates [81]. By interception of the cation with water we arrive at presilphiperfolan-8β-ol (31) Dickschat and co-workers reported an example for a ring contraction during the biosynthesis of sodorifen (32) [82]. The cyclisation is triggered by the C

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

• ]. In 2018, Kota and Sreevani prepared spirobarbiturates via a Mo(CO)6-catalyzed intermolecular [2 + 2 + 2] cycloaddition of propargyl halides with dipropargylbarbituric acid [24]. Almeida and colleagues described the formation of spiroindoline barbiturates via thermal rearrangement of 2,1-benzisoxazole

• determines cell motility, and its structural organization can serve as an indicator of the metastatic potential of tumor cells [63][64][65]. The presence of stress fibers and filopodia-like protrusions were used to evaluate the Sk-mel-2 cells' actin cytoskeleton structure after their co-incubation with spiro

• -fused adducts 4f, 4g, 4i, 4k, and 4l. Confocal microscopy showed that co-incubation of Sk-mel-2 cells with adducts 4f, 4g, 4i, 4k, and 4l led to significant changes in the structure of their actin cytoskeleton resulting in stress fibers disappearance (granular actin was found in the cytoplasm of up to

Arene activation via π-bond localization: concepts and opportunities

• Paul Meiners,
• Julian J. Melder and
• Tobias Morack

Beilstein J. Org. Chem. 2026, 22, 257–273, doi:10.3762/bjoc.22.19

• –Alder reactions with several electron-deficient dienes, furnishing distinctive methano-bridged structures (Figure 3C) [32][33][34][35]. Similarly, small cyclophanes are known to act as reactive dienes in Diels–Alder chemistry [36][37]. More recently, Lu and co-workers reported the unusually facile

• chemical literature, underscoring the potential of this strategy as a powerful platform for molecular discovery and medicinal chemistry. A similar strategic approach was utilized by Harman and co-workers to transform η2-coordinated anisole into a library of 3,6-substituted cyclohexenes with distinct

• early example was reported by Stille and co-worker in 1978, who elegantly demonstrated the formation of an η3-benzyl–palladium complex via oxidative addition of Pd(0) to a benzyl halide (Scheme 5C) [73]. Detailed stereochemical and NMR analyses revealed a temperature- and solvent-dependent equilibrium

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

• reactions catalyzed by diverse agents (Scheme 1). For instance, in 2013, Shi et al. described a three-component reaction involving 4-hydroxyquinolin-2(1H)-one, an aromatic aldehyde, and Meldrum’s acid, catalyzed by ʟ-proline under heating [37]. In the same year, Kurosh Rad-Moghadam and co-workers developed

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

• Ruiyan Wang Yunan Wu Sendelta International School, Shenzhen 518038, China Chongqing Institute of Green and Intelligent Technology, Chinese Academy of Sciences, Chongqing 400014, China New Materials Research Institute of CASCHEM (Chongqing) Co., Ltd, Chongqing 400714, China 10.3762/bjoc.22.16

• Technology Co., Ltd.; 3-(9H-carbazol-9-yl)phenylboronic acid (5) was obtained from Sukailu Co., Ltd.; glacial acetic acid, anhydrous sodium sulfate, dichloromethane, n-hexane, ethanol, chloroform, and tetrahydrofuran were supplied by Guangzhou Chemical Reagents Co., Ltd. All reagents were used as received