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Search for "ligands" in Full Text gives 1001 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.
Kinetic resolution of racemic planar-chiral vinylcymantrenes by molybdenum-catalyzed asymmetric metathesis dimerization
Beilstein J. Org. Chem. 2026, 22, 568–574, doi:10.3762/bjoc.22.42
- in Figure 2) likely inhibits the effective interaction of the substrate with the chiral catalyst, resulting in highly enantioselective kinetic resolution. Cymantrene is far less electron-poor than ferrocene due to the presence of the three carbonyl ligands, which are strong π-acids, on the manganese
Molecular tweezer–peptide conjugates disrupt the protein–protein interaction between survivin and histone H3 essential in mitosis
Beilstein J. Org. Chem. 2026, 22, 557–567, doi:10.3762/bjoc.22.41
- crystal (Figure 4 and Supporting Information File 1, Figure S12). Lys-121, on the other hand, is buried in a crystal contact. Thus, the crystal packing forces together with putatively competing ligands (see below) can apparently compete successfully with the tweezer that is most likely attached to Lys-121
Experimental and DFT studies on the regioselective methanolysis of 5-azido-9-oxabicyclo[6.1.0]nonan-4-yl 4-nitrobenzoate isomers
Beilstein J. Org. Chem. 2026, 22, 547–556, doi:10.3762/bjoc.22.40
- , pharmaceutical compounds, and chiral ligands. The Lewis acid-catalyzed ring-opening reaction of cyclohexene oxide by MeZH (Z = O, S, and NH) is well known [20]. However, studies on large-sized bicyclic epoxides remain relatively limited in the published literature. In our previous study, we performed the ring
Synthesis and uranyl(VI) extraction performance of a calix[4]pyrrole–tetrahydroxamic acid receptor
Beilstein J. Org. Chem. 2026, 22, 486–494, doi:10.3762/bjoc.22.36
- ligands can display significantly enhanced binding toward uranyl relative to their linear hydroxamic acid counterparts, emphasizing the beneficial role of structural organization in uranyl chelation [35]. This beneficial role of pre-organization of chelating groups within one molecule was also highlighted
- pH 2 and pH 3, the extraction efficiencies remain overall comparable within experimental uncertainty, suggesting that uranyl uptake is already near maximal in this acidic region. This behavior is consistent with previous studies in which ligands displayed high uranyl uptake within an optimal pH
- window. For instance, calix[4]arene-based 8-hydroxyquinoline ligands showed nearly quantitative extraction of uranyl between pH 4 and 9, with efficiency decreasing under more acidic conditions [67]. Likewise, phosphoramide-functionalized magnetic nanoparticles showed high uranyl adsorption (80–95
Synthesis of a HDAC inhibitor–nanogold probe for cryo-EM visualization in class I HDAC co-repressor complexes
Beilstein J. Org. Chem. 2026, 22, 480–485, doi:10.3762/bjoc.22.35
- , specifically Monoamino-Nanogold® 1.4 nm purchased from Nanoprobes) for our probe design. Au–NH2 consists of a gold cluster of eleven gold atoms coordinated by trisarylphosphine ligands with a diameter of 1.4 nm. One of the trisarylphosphine ligands contains the 3-aminopropylamido group, allowing for
Recent advances in the stereoselective synthesis of distal biaxially chiral molecules
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
- chiral scaffolds, which arise from hindered rotation between two planes connected by a single bond, have attracted increasing attention due to their widespread applications in chiral ligands, organocatalysts [1], and functional materials [2], making them highly valuable molecular frameworks in organic
- ligands (Scheme 3) [44]. The resulting catalysts 18 demonstrated remarkable efficiency in the asymmetric transfer hydrogenation of quinoline derivatives. Along similar lines, Zhang and co-workers introduced an additional axial chirality element into a ligand framework, affording a pair of diastereomeric
Synthesis and anti-cancer activity of naphthalimide–organylselanyl conjugates
Beilstein J. Org. Chem. 2026, 22, 416–435, doi:10.3762/bjoc.22.29
- 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
- ), hydrogen bonding (Met769), carbon–hydrogen bonding (Thr766), π–anion (Asp831), π–σ (Leu694), amide–π (Met769), alkyl (His781), and π–alkyl (Val702, Ala719, Leu768, Leu820). These results confirm that both ligands are well accommodated within the binding pocket of EGFR tyrosine kinase, with compound 7
- site interactions to those observed for erlotinib. Both erlotinib and the synthesised ligands formed a hydrogen bond interaction with Met769. The synthesised ligands have a greater ability to form an interaction with the active (1M17) tyrosine kinase domain of EGFR. Comparative binding interaction of
Arene activation via π-bond localization: concepts and opportunities
Beilstein J. Org. Chem. 2026, 22, 257–273, doi:10.3762/bjoc.22.19
- of the archetypal pentaammineosmium(II) system prior to discussing synthetic utility (Figure 6). The five ammine ligands, strong σ-donors with negligible π-interaction, combined with the d6 configuration render the Os(II) center highly electron-rich and an exceptional π-base [43]. This electronic
- configuration promotes strong binding to π-acidic ligands, effectively compensating for the loss of aromaticity upon η2-coordination to arenes, while disfavoring oxidative addition due to geometric constraints of the octahedral complex. The resulting η2-arene complexes, encompassing both arenes and heteroarenes
- (Figure 6C), so suitable aromatic ligands are limited to those lacking strongly π-acidic functional groups, e.g., alkenes, alkynes, aldehydes, certain ketones, and nitriles. Lewis-basic heteroarenes, such as pyridines or imidazoles, tend to coordinate via nitrogen instead, disfavoring η2-binding (Figure
Screwing the helical chirality through terminal peri-functionalization
Beilstein J. Org. Chem. 2026, 22, 205–212, doi:10.3762/bjoc.22.14
- another important type of chirality, where the chirality is controlled by restricted rotation among an axis. These types of molecules play an important role as chiral ligands in organic synthesis, i.e., BINOL, BINAP, etc. [9][10][11]. Another form of chirality, where chirality depends on a constrained
- asymmetric synthesis, where they serve as chiral ligands and organocatalysts, delivering high enantioselectivities [17][18]. Their tunable HOMO–LUMO gaps and controlled π–π interactions, is key to the use of helicenes in molecular electronics and organic semiconductors as well. Helicenes function as active
Improved synthesis and physicochemical characterization of the selective serotonin 2A receptor agonist 25CN-NBOH
Beilstein J. Org. Chem. 2026, 22, 175–184, doi:10.3762/bjoc.22.11
- agonists to study the effects of solely activating this key receptor [4]. 25CN-NBOH (1) was reported in 2014 as part of a series of ligands in the search for selective 5-HT2AR agonists [5]. Subsequently, it has been used and characterized extensively as a tool for investigations into the effects of
Design and synthesis of an axially chiral platinum(II) complex and its CPL properties in PMMA matrix
Beilstein J. Org. Chem. 2026, 22, 143–150, doi:10.3762/bjoc.22.7
- , pincer-type platinum(II) complexes have attracted particular attention, owing to the structural robustness imparted by tridentate chelating ligands and their excellent luminescent properties [12][13][14][15][16][17]. These complexes have been widely investigated, not only for practical application but
- arrangement of several molecules in the aggregated state. To expand the scope of chirality in metal complex chemistry with pincer ligands and to facilitate the design of next-generation CPL-active materials, alternative chiral motifs beyond point chirality are highly desirable. Herein, we report the design
Total synthesis of natural products based on hydrogenation of aromatic rings
Beilstein J. Org. Chem. 2026, 22, 88–122, doi:10.3762/bjoc.22.4
- rings becomes achievable, enabling access to reduced products with well-defined configurations [38]. Although the repertoire of ligands capable of exerting precise stereocontrol remains limited, each provides distinct advantages that suit different metals and reaction conditions. From the perspective of
- in the presence of metal catalysts including Pd or Ir and different ligands. In 2021 and 2022, Wang and co-workers reported two impressive hydroboration–hydrogenation reactions catalyzed by FLP (triarylphenylborane) that reduced pyridine compounds 11 or 15 to dihydropyridine compounds 12 or chiral
- reported for the first time the reduction of 1,3-disubstituted isoquinoline compounds 45 to trans-quinoxalines 46 (Scheme 6) [56]. By using iridium catalysts and commercially available chiral JosiPhos ligands, a batch of enantioriched trans-tetrahydroisoquinolines could be prepared efficiently and
Synthesis and applications of alkenyl chlorides (vinyl chlorides): a review
Beilstein J. Org. Chem. 2026, 22, 1–63, doi:10.3762/bjoc.22.1
- is generated in situ and likely present only in trace amounts. All our attempts to accelerate the reaction through addition of various mono- and bidentate phosphorus ligands were unsuccessful. A similar trend was observed with NEt3, which afforded optimal yields at 20–30 mol % loading (not shown
- demonstrated that the use of 4 equivalents of 1,1-dichloroethylene in combination with XPhos or JohnPhos ligands enabled monoselective cross-coupling with alkenyl- and arylboronic acids (Scheme 54B) [184]. Though mechanistically not related it is noteworthy that diazonium salts couple efficiently with alkenyl
Isoorotamide-based peptide nucleic acid nucleobases with extended linkers aimed at distal base recognition of adenosine in double helical RNA
Beilstein J. Org. Chem. 2025, 21, 2513–2523, doi:10.3762/bjoc.21.193
- linker are highlighted in red. Sequences for RNA hairpins and PNA ligands used for binding studies. Major-groove view of hydrogen-bonding interactions in the (A) Db1*U–A triplet, (B) Db2*U–A triplet, (C) Db2*C–G triplet, and (D) Db3*U–A triplet. Carbon, hydrogen, oxygen, and nitrogen are labelled in
Catalytic enantioselective synthesis of selenium-containing atropisomers via C–Se bond formations
Beilstein J. Org. Chem. 2025, 21, 2447–2455, doi:10.3762/bjoc.21.186
- Atropisomers are not only prevalent in biologically active natural products and pharmaceuticals, but they have also garnered increasing attention for their effectiveness as ligands and catalysts in the field of catalytic asymmetric synthesis. Asymmetric catalysis serves as a key strategy for the
- compounds can participate in asymmetric synthesis reactions and construct chiral molecules with specific stereoconfiguration, which is particularly critical for drug synthesis [9]. In the field of organic catalysis, chiral organic selenium-containing compounds can be used as chiral ligands or catalysts to
Enantioselective radical chemistry: a bright future ahead
Beilstein J. Org. Chem. 2025, 21, 2283–2296, doi:10.3762/bjoc.21.174
- catalysis affords the dual advantages of introducing stereochemical discrimination on both the radical and the trap via chiral ligands. Early research on parameters governing stereoselectivity in radical reactions was achieved with the help of radicals or radical traps appended with chiral auxiliaries. The
Pathway economy in cyclization of 1,n-enynes
Beilstein J. Org. Chem. 2025, 21, 2260–2282, doi:10.3762/bjoc.21.173
- substrate class. Through mechanistic-guided modulation of catalysts, solvents, ligands, and angle strain, this approach achieves unprecedented reaction pathway control while demonstrating superior temporal and step efficiency compared to conventional methods. The work establishes a sustainable framework for
- components such as solvents, catalysts, ligands and so on. Unlike traditional “one-to-one” reactions, pathway-controlled “one-to-many” transformations synthesize multiple products from single intermediates, dramatically reducing preparation time and reagent requirements (Scheme 1b). As an exceptionally
- heterocyclic scaffolds, which established a versatile platform for synthesizing structurally diverse indoline frameworks. Ligand-controlled cyclization of 1,n-enynes The core function of catalyst ligands lies in their ability to precisely modulate catalyst performance through electronic and steric effects. The
Research towards selective inhibition of the CLK3 kinase
Beilstein J. Org. Chem. 2025, 21, 2250–2259, doi:10.3762/bjoc.21.172
- affinity of ligands towards the CLK3 kinase. It is based on the lysine 241 which is present only in CLK3, while the three others (CLK1, 2, and 4) have apolar leucine in this position. Thus, by grafting an extra benzoic acid on a molecule previously established as having low activity on CLK3 (DB18), we have
Pd-catalyzed dehydrogenative arylation of arylhydrazines to access non-symmetric azobenzenes, including tetra-ortho derivatives
Beilstein J. Org. Chem. 2025, 21, 2234–2242, doi:10.3762/bjoc.21.170
- regioselectivity issues, multistep procedures, and limited applicability to tetra-ortho-substituted structures. Herein, we describe a direct, one-pot Pd-catalyzed dehydrogenative C–N coupling between aryl bromides and arylhydrazines to access non-symmetric azobenzenes. The use of bulky phosphine ligands and
- the presence of water, highlighting its robustness. Keywords: azo compounds; cross-coupling; domino catalysis; palladium; phosphine ligands; Introduction Azobenzenes are a widely studied class of compounds known for their distinctive photoresponsive properties, rendering them valuable in a variety
- (allyl)2 in DME with strong base (Cs2CO3) favors C–N-bond coupling, which may yield products resulting from arylation at either the terminal or internal nitrogen atoms. The selectivity can be influenced by the steric hindrance of the phosphine ligands and/or the substrates. Once N,N-diarylhydrazine is
Electrochemical cyclization of alkynes to construct five-membered nitrogen-heterocyclic rings
Beilstein J. Org. Chem. 2025, 21, 2173–2201, doi:10.3762/bjoc.21.166
- reaction mechanisms are disclosed if available. Keywords: alkyne; catalysis; cyclization; electrochemistry; five-membered ring; Introduction Organic five-membered rings, an essential class of organic compounds, not only are frequently used as important starting materials, intermediates or ligands in
- , this protocol was an efficient and sustainable approach to synthesize 2,3′-biindolyl atropisomers and could be potentially applied in manufacture of functional materials, bioactive molecules and chiral ligands. Construction of isoindolinones and indolizines An electrochemical and copper-catalyzed
Discovery of cytotoxic indolo[1,2-c]quinazoline derivatives through scaffold-based design
Beilstein J. Org. Chem. 2025, 21, 2062–2071, doi:10.3762/bjoc.21.161
- exceptional potential as ligands targeting secondary structures of nucleic acids, particularly G-quadruplexes (G4) [21][22]. The indolo[1,2-c]quinazolin-6(5H)-one scaffold 1 exemplifies this design principle, with its rigid polycyclic framework mimicking topologies of established DNA/RNA-interactive molecules
Photochemical reduction of acylimidazolium salts
Beilstein J. Org. Chem. 2025, 21, 1973–1983, doi:10.3762/bjoc.21.153
- ; carbonyls; NHCs; photochemistry; reduction; Introduction The introduction and exploration of N-heterocyclic carbenes (NHCs) ranks among the most important developments in chemistry research of the last 30 years [1][2][3]. In addition to their numerous valuable roles as ligands, including for important
Enantioselective desymmetrization strategy of prochiral 1,3-diols in natural product synthesis
Beilstein J. Org. Chem. 2025, 21, 1932–1963, doi:10.3762/bjoc.21.151
- reactions, chemists have developed a series of catalysts composed of transition-metal cores and chiral ligands, which have been applied to various asymmetric reactions [50][51][52]. Compared to the enzymatic methods, the transition-metal-catalyzed approach may provide an advantage to access both enantiomers
- enantioselective desymmetrization of prochiral 1,3-diols within complex structures can be realized using organometallic catalysts composed of copper or zinc salts and different types of chiral ligands. In general, the ability to control the stereoselectivity of the product by using the enantiomer of the ligand in
Stereoselective electrochemical intramolecular imino-pinacol reaction: a straightforward entry to enantiopure piperazines
Beilstein J. Org. Chem. 2025, 21, 1897–1908, doi:10.3762/bjoc.21.147
- applications in the preparation of chiral ligands. Keywords: chiral piperazines; electrosynthesis; flow chemistry; green chemistry; imino-pinacol coupling; Introduction Vicinal diamines represent a highly valuable class of compounds that, over the past decades, have found widespread application in natural
- products, agrochemicals, and pharmacologically active compounds. Enantiomerically pure 1,2-diamines and their derivatives are also increasingly used in stereoselective synthesis, particularly as chiral auxiliaries or as ligands for metal complexes in asymmetric catalysis [1]. Metal-based reductants
- scaffolds that are commonly used as chiral ligands. In this context we report the development of a more sustainable method – which avoids the use of lead bromide or lead electrodes – employing an undivided cell with two glassy carbon electrodes for the electroreductive intramolecular coupling of aromatic
Chiral phosphoric acid-catalyzed asymmetric synthesis of helically chiral, planarly chiral and inherently chiral molecules
Beilstein J. Org. Chem. 2025, 21, 1864–1889, doi:10.3762/bjoc.21.145
- leveraging the synthesized enantioenriched aza[6]helicene 29a and tetrahydro[6]helicene 30a as chiral building blocks, a series of helically chiral organocatalysts and ligands could be easily prepared, such as the helically chiral pyridine N-oxide 31a and helically chiral monophosphine ligands 31b,c, whose
- versatility of this method in the asymmetric synthesis of diverse chiral molecular structures. Substituted [2.2]paracyclophanes represent another class of conformationally rigid, planarly chiral molecules, which have emerged as versatile scaffolds for developing chiral catalysts, ligands and functional
- DDD products 64e. Moreover, the authors showcased the facile derivatization of dimethoxy-substituted chiral DDD 64f into various DDD-based chiral ligands, such as the phosphoramidites 65, phosphoric acid as well as monophosphine ligands and diphosphine ligands 66. Notably, the applications of these
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