One-pot four-component sequential synthesis of S-alkyl dithiocarbamates using lipase as a biocatalyst

• Mansour Shahedi,
• Pargol Tahmasebi pour and
• Zohreh Habibi

Beilstein J. Org. Chem. 2026, 22, 1048–1056, doi:10.3762/bjoc.22.83

• nucleophilic addition reaction with dithiocarbamate anions, which are generated in situ by reacting CS2 with amines. This sequence successfully yields 15 derivatives of S-alkylated dithiocarbamates with high to excellent yields ranging from 69% to 96%. Keywords: biocatalysis; dithiocarbamate; four-component

• a four-component reaction with benzaldehyde derivatives, aryl methyl ketones, amines, and carbon disulfide to form S-alkyl dithiocarbamates. However, when acetone was used as the fourth component in this reaction, no dithiocarbamate product was formed, and instead, benzylidene acetone was identified

• formed from an amine and carbon disulfide, without isolation of intermediates. Under mild reaction conditions, 15 derivatives were obtained in good to excellent yields. Beyond the preparation of the target compounds, this study highlights the potential of lipase catalytic promiscuity in sequential

Synthesis of novel 1,2,4-oxadiazole-isoxazoline hybrids and their in silico potential with adenosine receptors

• Pshtiwan S. Mohammed,
• Mohammed K. S. Dalo,
• Onur C. Yazıcı,
• Muhammet Yildirim and
• Akın Sağırlı

Beilstein J. Org. Chem. 2026, 22, 1033–1047, doi:10.3762/bjoc.22.82

• –97%) and fully characterized by IR, NMR, and HRMS analyses. The reactions exhibited high regioselectivity, exclusively affording 5-isoxazoline derivatives, while substituent effects played a decisive role in modulating reaction efficiency. In silico studies revealed that all hybrids 7a–ay display

• amide functional groups [1][2][3][4][5]. 1,2,4-Oxadiazole derivatives interact with various receptors as agonists or antagonists, demonstrating a wide spectrum of biological activities including anti-inflammatory, anticancer, antidepressant, anti-HIV, antifungal, and anticonvulsant properties [6][7][8

• , such as sulfisoxazole, oxacillin, and acivicin, have been clinically utilized for many years [21][22][23][24][25][26][27][28] (Figure 1). The synthesis of 1,2,4-oxadiazole derivatives can be achieved through various efficient methods, such as the cyclocondensation of amidoximes with carbonyl compounds

Semisynthesis, characterisation, and antibacterial evaluation of a novel lecanoric acid-derived amide library

• Ethan D. Abbott,
• Sasha Hayes,
• Jonathan M. White,
• Bernd H. A. Rehm and
• Rohan A. Davis

Beilstein J. Org. Chem. 2026, 22, 1023–1032, doi:10.3762/bjoc.22.81

• metabolites that included divaricatic acid (2), orcinol (3), orsellinic acid (4), and methyl orsellinate (5). Parallel solution-phase synthesis using amidation chemistry on the abundant scaffold 1 afforded a series of novel amide derivatives 6–13 in high purity (>95%) and low to moderate yields (12–53%). All

• products and their semisynthetic derivatives. Owing to the Davis group’s ongoing interest in the semisynthesis of unique and rare biodiscovery screening libraries based on Australian natural products [10][11][12][13][14], a locally collected lichen, Parmotrema tinctorum, was selected for chemical

• the aromatic moiety was established through HMBC and ROESY correlations. Key COSY, HMBC, and ROESY correlations are shown below in Figure 4. Owing to the Davis group’s interest in discovering new natural products or derivatives with antibacterial properties, all compounds 1–13 were assessed via a

Synthesis and optical resolution of 4,5-diaminohomoadamantane: a promising scaffold for chiral ligands and bioactive compounds

• Polina A. Man’kova,
• Vadim A. Shiryaev,
• Olga S. Podlipnova,
• Marat M. Khisyamov,
• Dmitry S. Nikerov,
• Alexander N. Reznikov and
• Yuri N. Klimochkin

Beilstein J. Org. Chem. 2026, 22, 1013–1022, doi:10.3762/bjoc.22.80

• CAM-B3LYP functional and the 6-311G++(2d,2p) basis set with solvation by CH2Cl2 in the SMD model on the base of conformational analysis. Catalytic systems based on (4R,5R)-4,5-diaminohomoadamantane derivatives exhibited low to moderate asymmetric induction in Henry and Michael reactions. These results

• , a few examples of homoadamantane derivatives showing pronounced biological activity are known. More than 40 homoadamantane polyprenylated acylphloroglucinols have been isolated from Hypericum plants [54][55][56]. Among them, hyperacmosins A and B showed a protective effect in paracetamol-induced

Z-Selective semihydrogenation of alkynes via Ni/Lewis acid synergistic catalyzed system using DMF as hydrogen source and solvent

• Lei Kang,
• Haifeng Gao and
• Luo Yang

Beilstein J. Org. Chem. 2026, 22, 1004–1012, doi:10.3762/bjoc.22.79

• and nickel catalysts further suggests its potential as a combined solvent and hydrogen donor in a synergistic catalytic manifold [43][44]. Related amide derivatives, such as formamide, have also been employed as safe cyanide sources or hydrogen-donor precursors, offering useful precedents for their

• -withdrawing groups (trifluoromethyl 2f; halogens 2g–o), and even an amide moiety (2p) were smoothly converted to the corresponding (Z)-stilbene derivatives in good to excellent yields (70–95%), with uniformly high stereoselectivity (Z/E = 97:3 to >99:1). The reaction demonstrated excellent functional group

• mol % Zn(OAc)2·2H2O, DMF, 150 °C, 24 h), substrates bearing methyl (4b), methoxy (4c), and halogen (F for 4d, Cl for 4e, Br for 4f) substituents were smoothly converted to the corresponding styrene derivatives in 64–68% yields. Both electron-donating groups (methyl, methoxy) and halogen functional

Rh(III)-catalyzed chelation-assisted C–H activation/annulation of 2-arylimidazolines with cyclic diazo-1,3-dicarbonyl compounds: a novel approach to tetracyclic annulated derivatives of 2,3-dihydroimidazo[2,1-a]isoquinoline

• Ivan Lyutin,
• Grigory Kantin,
• Olga Bakulina and
• Dmitry Dar'in

Beilstein J. Org. Chem. 2026, 22, 997–1003, doi:10.3762/bjoc.22.78

• for the creation of more potent medications and the hunt for novel biologically active compounds. One important group of these are imidazoline derivatives since they are well known as pharmacophores [1] for adrenergic and imidazoline receptors. Imidazolines have found utility in the development of

• synthesizing imidazolines [7][8], but access to their annulated derivatives is still very limited despite many promising results on their bioactivity. For example, several derivatives of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines (Figure 1, 1) have demonstrated antitumor [9][10][11], anti-inflammatory, and

• immunosuppressive activity. The latter was used to develop antiasthmatic, pulmonary, and anti-allergy agents acting as platelet-activating factor receptor (PAF-R) antagonists [12][13]. Derivatives with X = H were accessed only via lithiation of 2-(o-tolyl)imidazolines followed by condensation with aromatic esters

Novel macrocycles: from synthesis to supramolecular function

• Veronica Iuliano,
• Carmen Talotta,
• Margherita De Rosa,
• Paolo Della Sala,
• Konrad Tiefenbacher,
• Pablo Ballester and
• Carmine Gaeta

Beilstein J. Org. Chem. 2026, 22, 982–985, doi:10.3762/bjoc.22.76

• application potential of macrocyclic chemistry, their further development relies on access to versatile and selectively functionalizable scaffolds. In this context, Vatsouro and co-workers [40] report efficient methodologies for accessing heteromultifunctional calix[4]arene derivatives. Through carefully

• derivatives that assemble into homo- and heterodimeric supramolecular capsules. This work establishes adaptable synthetic platforms for the preparation of increasingly complex supramolecular architectures. The development of such multifunctional systems can also help address major environmental challenges

Electrochemical reduction of unsaturated carbon–carbon bonds via 3d transition-metal catalysis

• Geon Kang,
• Minki Jeon,
• Pooja Kumari Jat,
• Cheoljae Kim and
• Isaac Choi

Beilstein J. Org. Chem. 2026, 22, 955–981, doi:10.3762/bjoc.22.75

• , and the successful late-stage electrohydrogenative functionalization of structurally complex molecules and drug derivatives further underscored the practical applicability of this strategy in medicinal chemistry contexts. To probe the involvement of catalytically relevant Fe–H species, radical probe

• exhibits a broad substrate scope, high efficiency, excellent functional-group tolerance, and consistently high levels of deuterium incorporation (Scheme 5Bi) [100][101]. Notably, the transformation proceeds efficiently with derivatives of biologically active molecules, such as serine and niflumic acid

• , the desired succinic acid derivatives were obtained. Importantly, this efficient conversion was observed only in the presence of the mediator; in its absence, product yields were markedly diminished and substantial amounts of starting material remained unreacted. According to the proposed mechanism

Synthesis of sterically shielded piperidine nitroxides via acid-catalyzed heterocyclization of β-aminoketone derivatives with ketones

• Mark M. Gulman,
• Yurii I. Glazachev and
• Sergey A. Dobrynin

Beilstein J. Org. Chem. 2026, 22, 948–954, doi:10.3762/bjoc.22.74

• -tetraethylpiperidine (TEEPONE). Keywords: heterocyclization; piperidine nitroxide; TEEPONE synthesis; Introduction Since their discovery in 1959 by Lebedev and Kazarnovsky, stable nitroxides of the piperidine series (2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) derivatives) hold a prominent position as compounds of

• radicals are based on approaches employing either the tetraethyl analog of phorone or acetonine [11][15][17][18] or the desulfurization of dispirothiapyranone derivatives [19][20][21][22]. Consequently, the structural diversity of radicals bearing acyclic substituents is practically limited to derivatives

• nitroxides 7a–d in 50–80% overall yield from piperidines 5a,b (Scheme 3). The structures of nitroxides 7a–d were confirmed by 1H NMR spectroscopy of their amine derivatives, obtained via Zn/CF3COOH reduction in CD3OD, following a reported procedure [37]. The full line-shape analysis of the 1H NMR spectra for

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

• -Michael addition [13][14][15][16][17][18]. In such cases, the reaction provides direct access to β-amino carbonyl derivatives and related motifs that serve as versatile intermediates in synthetic and medicinal chemistry. Despite its conceptual simplicity, catalytic hydroamination remains challenging. This

• using an inexpensive CuCl catalyst in combination with electron-donating phosphine ligands (L1, L2) or NHC salts (L3, L4) and KOt-Bu [37]. Various aromatic amines and heteroaromatic N–H nucleophiles reacted efficiently with electron-deficient alkenes 2, such as vinyl sulfones, acrylonitrile derivatives

• significantly affecting the reaction efficiency. In addition to simple anilines, diverse heteroaromatic amines including indole, pyrrole, triazole, carbazole, and imidazole derivatives participated effectively in the copper-catalyzed conjugate addition, providing the corresponding β-amino products 3 in high

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

• challenging synthesis of 5,6-carboxylated SiR derivatives, which are essential intermediates for bioconjugation. Here, we report a practical CO2-mediated strategy for the synthesis of 5,6-carboxylated SiRs from brominated SiR precursors via lithium–halogen exchange and direct carboxylation. Using n-BuLi and

• readily available CO2, this method delivers carboxylated SiR derivatives in 60–93% yields while avoiding the use of t-BuLi, toxic CO, and expensive palladium catalysts. In addition, the crude carboxylation mixtures can be directly subjected to amide coupling without chromatographic purification, enabling

• makes SiRs highly attractive as fluorogenic probes for precise super-resolution imaging by enabling target-specific recognition and significantly improving signal-to-noise ratio (SNR). In addition, hydroxymethyl-substituted SiR derivatives, including HMSiR [30][31] and Aze-HMSiR [32][33][34], can

Palladium-catalyzed benzocyclization reactions of quinoline-2-carboxamides via sequential C–H/N–H functionalization

• Shoichi Sugita,
• Kentaro Okano and
• Atsunori Mori

Beilstein J. Org. Chem. 2026, 22, 905–914, doi:10.3762/bjoc.22.71

• intriguing moiety in biologically active compounds (e.g., natural products used for medicines, quinine, and quinidine [5][6][7]) and synthesized pharmaceutical agents (e.g., quinolone antibiotics [8]). Moreover, quinoline-2-carboxamide derivatives are used as ligands in organic synthesis owing to their high

• preparation of annulation precursors through o-brominated aniline derivatives [36][37][38][39][40][41]. Furthermore, the reported methodologies for synthesizing N-heterocycle-fused lactams are characterized by either low efficiency or protracted processes [42][43]. On the other hand, benzocyclization

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

• (Scheme 6). However, attempts to cyclize them using the benzoyl group to form 4H-furo[3,2-b]pyrrole derivatives were unsuccessful. Triflate 7a is obtained from pyrrole 5a by treatment with Tf2O in 85% yield, but it proved inert in the Suzuki reaction with 4-chlorophenylboronic acid and 2-(4,4,5,5

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

• synthesis, neurotransmitter function, and regulation of acid-base balance, metabolic intermediates, and promotion of nutrient absorption [4]. Therefore, the synthesis of substituted glutamic and pyroglutamic acid derivatives is vital to medicinal chemistry. In our previous reports, we have synthesized a

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

• task [25][26][27]. The electronic character of these intermediates, especially for boronic ester derivatives that allow coordination between oxygen atoms and the metal counterion, complicates predictable stereochemical outcome. Developing strategies to harness the exceptional nature of these carbanions

• lithium derivatives. Reactivity of α-boryl lithium intermediates 5 possessing alkyl substituents at the allylic position. Effect of the nature of the substituent R3 on the diastereoselectivity. Mechanistic hypothesis to rationalize the diastereoselectivity. Supporting Information Supporting Information

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

• corresponding thioether 1 (AE = 2.45), both containing an isopropyl substituent. However, these AE values exceeded that of 3,5-DTBC, indicating enhanced neutralizing activity of the sulfur-containing derivatives. The ABTS assay is one of the most widely used methods for assessing the antioxidant capacity of

• values observed for compounds bearing isopropyl and tert-butyl substituents. Notably, sulfoxide 1a (isopropyl) showed enhanced antiradical activity compared to its thioether precursor, while for most other derivatives the activity decreased upon oxidation of sulfur. The combination of a primary

Synthesis and structural elucidation of a novel bis-spirooxindole from isatin and ethylenediamine

• Irene Moreno-Gutiérrez,
• Josefa L. López-Martínez,
• Sonia Berenguel-Gómez,
• Irene Torres-García,
• Duane Choquesillo-Lazarte,
• Manuel Muñoz-Dorado,
• Miriam Álvarez-Corral and
• Ignacio Rodríguez-García

Beilstein J. Org. Chem. 2026, 22, 813–820, doi:10.3762/bjoc.22.63

• carbonyl group with a γ-lactam system, which enables participation in a wide range of nucleophilic additions, condensations, and cyclizations [7]. As a result, isatin has proven to be a particularly powerful synthon for the construction of 2-oxindole derivatives, including a large variety of spiro-fused

• , multicomponent systems combining isatin derivatives with diamines have been reported to furnish bis-spirocyclic architectures like 21 without detectable formation of the corresponding diimines 22 [20] (Scheme 3). Collectively, these precedents demonstrate that condensations of isatin with bifunctional nitrogen

• geometrical isomers (E/E, E/Z, Z/Z). These spectroscopic data are in agreement with those of previously described diiminoisatin derivatives [21]. When the reaction was carried out with an excess of ethylenediamine, a completely different product was obtained (Scheme 4b). Refluxing an ethanol solution of

Knoevenagel condensation of 4,5- and 1,8-diazafluorenes

• Darya S. Cheshkina,
• Christina S. Becker,
• Alina A. Sonina and
• Maxim S. Kazantsev

Beilstein J. Org. Chem. 2026, 22, 803–812, doi:10.3762/bjoc.22.62

• with ketones resulted in unique di(pyridin-2-yl)methylene)-9H-diazafluorenes being electron-deficient ligands and functional materials. Keywords: acidic conditions; diazafluorene; diazafluorenylidene; Knoevenagel condensation; protonation; Introduction Diazafluorenylidene derivatives were reported to

• for their synthesis involves coupling reactions of diazafluoren-9-one [4][6][7] or diazafluoren-9-diazomethane [17][18] with thiones yielding the products in moderate yields (20–70%). However, these routes require the preliminary synthesis of malodorous thiones and diazomethane derivatives from the

• malononitrile or acetonitrile derivatives [14][19][20]. However, the use of diazafluorenes as the methylene component in condensation reactions remains underexplored. These reactions can be carried out under basic [13][21], acidic [3][5] or Lewis acid catalysis [15][22], but the corresponding literature

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

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

• a very useful tool to tune the thermal and optical properties, light-induced switching in particular. Monohalogen derivatives exhibited up to 93% E → Z photoconversion efficiency in solution, whereas the efficiency of dihalogen analogues is lower by 20%, which is ascribed to their nonplanar

• 1a vs 1b, 1c vs 1d; except for the bromine derivatives 1e and 1f where Ti is almost equal). The most pronounced difference was recorded for the chloro-substituted pair 1c and 1d (ΔTi = 41 °C). Electrochemistry The electrochemical behavior of azo-compounds 1a–f was investigated in 1,2-dichloroethane

• reverse reduction of the chemically modified oxidized form was recorded as a broad peak at significant undervoltage, especially for derivatives 1a–b and 1d–e. The electrochemical data suggest that the first oxidation and the first reduction processes are associated with different parts of the molecule

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

• , and to support a balanced gut microbiota [7]. In view of this pleiotropic role, FXR activation has emerged as a well-established pharmacological target for MASH [8]. Consequently, a diverse range of FXR agonists – categorized as bile acid derivatives, non-bile-acid steroidal agonists, non-steroidal

• FXR agonist, served as the lead compound for a series of derivatives, such as cilofexor (GS-9674). Unfortunately, these agonists have failed in clinical trials because of side effects such as itching or a failure to meet primary endpoints. Despite the failure of several FXR agonists to achieve the

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

• ]pyridine-2-carbaldehydes is reported. A Groebke–Blackburn–Bienaymé reaction between 2-aminopyridine derivatives, cyclohexyl isocyanide and glyoxylic acid in the presence of methanol and an acid catalyst gave the 2-ester derivatives that were reduced to give the corresponding alcohols. Mild Kornblum

• -chloroaniline. Alternative oxidation conditions such as PCC, IBX or T. versicolor laccase applied to the alcohols led only to oxidative ring-opening to give oxalamide derivatives, with no aldehyde being isolated. Keywords: 3-aminoimidazo[1,2-a]pyridine-2-carbaldehydes; Groebke–Blackburn–Bienaymé reaction

• found to act on targets in the central nervous system. For example, zolpidem (1) is used for the treatment of sleeping disorders, while alpidem (2), now discontinued due to safety concerns, was used for the treatment of anxiety (Figure 1). Other derivatives are currently under investigation for their

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

• matter of current interest. For example, derivatives of teasterone (3), compounds 4–11, and castasterone, compounds 12–14, with benzoyl function at C-22 (Figure 2) have been synthesized, and their bioactivities have been evaluated by BSIB, RLIT, and inhibition of root and hypocotyl elongation in A

• in Table 2. The data indicate that derivatives with a OH group at C-3 (TE analogs) are much more active than derivatives with a carbonyl group in this position (3-DT analogs). However, the addition of another OH group at C-2 (CAT analogs) increases the activity of analogs substituted with p-methyl

• . thaliana seedlings. In the former test the best biological effects were observed for the analogs with 2α,3α-dihydroxy function (castasterone derivatives) as compared to those obtained for analogs with 3β-hydroxy (teasterone derivatives) and 3-carbonyl function. This result confirms that the best activity

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

• derivatives with multiple chiral centers under high regio- and stereocontrol. Currently, strategies using azomethine ylides based on imino esters or α-amino acids with a variety of cyclic and acyclic carbonyl compounds dominate. Enantioselective (3 + 2) cycloaddition reactions of azomethine ylides obtained

• ]. 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

• -pyrrolizidine derivatives obtained from isatin, various α-amino acids and dipolarophiles is considered. This structural fragment plays an important role in biological processes, exhibiting antitumor activity, anti-HIV activity, anti-inflammatory, and, in some cases, analgesic effects. A 2016 review addressed

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

• approved by the FDA are derived from natural products, their derivatives, or synthetic mimetics inspired by natural compounds [5]. The traditional knowledge of native plants for medicinal purposes is invaluable, and there are ongoing investigations by many research groups from around the world that aim to

• Eremophila-derived specialized metabolites or semisynthetic derivatives has the potential to impact biodiscovery research. In this study, we investigated the chemistry of the seeds of Eremophila maculata for the first time. Seeds from the Eremophila genus have rarely been chemically investigated due to

• uniquely abundant plant part afforded two known phytochemicals, (+)-salicifoliol (1) [15][16] and (+)-pinoresinol (2) [17]. The abundant natural product 2 was used as a chemical scaffold for semisynthetic studies. At the same time, all derivatives were fully characterized utilizing spectroscopic and