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Search for "assembly" in Full Text gives 642 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.
Total synthesis of the capsular polysaccharide repeating unit towards the development of a glycoconjugate vaccine against Klebsiella pneumoniae ST512
Beilstein J. Org. Chem. 2026, 22, 821–827, doi:10.3762/bjoc.22.64
- assembly and subsequent functionalization of long oligosaccharide chains are hampered by their intrinsically low reactivity [29]. Overcoming these challenges relying on a linear strategy employing four key building blocks 1–4, we describe the first chemical synthesis of the hexasaccharide repeating unit
- ). Finally, protection of the hydroxy groups with benzyl ethers furnished building block 3 in 83% yield. With the building blocks in hand, the assembly of the hexasaccharide was pursued as outlined in Scheme 2. The synthesis commenced with the coupling of monosaccharides 1 and 2 promoted by NIS/TfOH followed
- -throughput screening, a series of analogues including di-, tri-, tetra-, and pentasaccharides were synthesized (Scheme 3). We utilized the intermediate products from the assembly of the hexasaccharide repeating unit 20. The protecting groups of disaccharide 13 were removed by treatment with sodium methoxide
Synthesis and structural elucidation of a novel bis-spirooxindole from isatin and ethylenediamine
Beilstein J. Org. Chem. 2026, 22, 813–820, doi:10.3762/bjoc.22.63
- , these results show that the reaction of isatin with ethylenediamine can be directed toward different structural outcomes depending on stoichiometry. Simple control of stoichiometry governs whether the system evolves through a conventional diimine pathway or diverges toward the assembly of a highly
Synthesis and biological evaluation of new brassinosteroid analogs with C-22 benzoate function
Beilstein J. Org. Chem. 2026, 22, 753–762, doi:10.3762/bjoc.22.57
- structurally and functionally comprehensive model system resolved by X-ray crystallography. Unlike BRL1 and BRL3, for which only monomeric ectodomain structures are available, the 4M7E structure enables modeling of the full receptor–co-receptor assembly required for the “molecular glue” mechanism involving
Synthesis of heterocycles based on azomethine ylides from α-amino acids (or amines) and carbonyl compounds
Beilstein J. Org. Chem. 2026, 22, 705–741, doi:10.3762/bjoc.22.55
- hypothesized that when ligand L8 is utilized, throughout the entire catalytic cycle both the nitrogen and phosphorus atoms of the ligand maintain their coordination to copper. The final product 16 is formed as a consequence of electron redistribution within the metal-ligand assembly, coupled with steric
Harnessing light energy with molecules
Beilstein J. Org. Chem. 2026, 22, 680–682, doi:10.3762/bjoc.22.52
- larger systems or smart materials [9]. Photoswitches are, for example, relevant functional units for information storage or molecular electronic devices. They can serve to control ion transport, molecular assembly/disassembly, or the relative movement of units within molecular machines. In a Review
Advantages of PROTACs in achieving selective degradation of homologous protein families
Beilstein J. Org. Chem. 2026, 22, 628–661, doi:10.3762/bjoc.22.49
- optimization often prioritizes the linker fragment, as its length and composition are critical determinants of target selectivity [39]. Recent evidence underscores the pivotal role of the linker in promoting the assembly of "positive cooperative" ternary complexes [40], wherein the linker participates in
Towards the targeted protein degradation of CK2: design and synthesis of CAM4066-based PROTACs
Beilstein J. Org. Chem. 2026, 22, 611–619, doi:10.3762/bjoc.22.47
- problems [6]. The ATP-site binder and αD-site binder fragments were prepared using literature procedures from the original development of 1. The modified linking portion containing the new secondary amine was incorporated into the general assembly 2 to afford a CAM4066-derived scaffold suitable for PROTAC
- 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
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
- ; protein–protein interaction; mitosis; X-ray crystallography; Introduction The fundamental process of mitosis is controlled by a very large protein complex called the kinetochore, formed by self-assembly from hundreds of single protein components [1]. For the intricate regulation of the various phases of
Modern synthetic pathways towards eribulin and its subunits
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
- 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
- and addition of vinylmagnesium bromide, 21 was received and dihydroxylated towards 22 in 5:1 dr. The second path towards 27 commenced with the assembly of 23 from 14 via Bn-protection, following oxidation and Horner–Wadsworth–Emmons (HWE) reaction (Scheme 3). Stereospecific vinylation with a Gilman
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
- assembly of complex distal biaxial architectures that are difficult to access via direct or stepwise axis formation alone. In 2019, Bertuzzi and co-workers achieved the first enantioselective synthesis of an axially chiral indole–quinoline system (Scheme 25) [64]. They employed a central-to-axial oxidative
- biaryl compounds. Highly enantioselective C–H arylation of heteroarenes. Synthesis of novel axially chiral N-arylcarbazole skeletons by the assembly of azidonaphthalenes and carbazoles through chiral phosphoric acid catalysis. Catalytic enantioselective synthesis of axially chiral polycyclic aromatic
Concept-driven strategies in target-oriented synthesis
Beilstein J. Org. Chem. 2026, 22, 451–454, doi:10.3762/bjoc.22.32
- complex organic architectures have witnessed remarkable achievements in recent years, continuously redefining the boundaries of creativity, efficiency, and practicality. On the other hand, it has been suggested that the field of complex molecular assembly is transitioning (or ought to transition) from an
Synthesis and anti-cancer activity of naphthalimide–organylselanyl conjugates
Beilstein J. Org. Chem. 2026, 22, 416–435, doi:10.3762/bjoc.22.29
- geometry around the selenium atom. The structure reveals the four distinct intermolecular interactions that facilitate the self-assembly in the crystal packing. The first is a chalcogen bonding interaction (Se···Se) [53], as shown in Figure 2b, in which one aryl selenide molecule linearly connects to
A mild and atom-efficient four-component cascade strategy for the construction of biologically relevant 4-hydroxyquinolin-2(1H)-one derivatives
Beilstein J. Org. Chem. 2026, 22, 244–256, doi:10.3762/bjoc.22.18
- , enabling the one-pot combination of three or more reactants to form multiple bonds in a single step [4][5][6][7][8]. This approach not only facilitates the rapid assembly of structurally complex and functionally diverse molecules, but also aligns with the principles of green and sustainable chemistry
- synthetic accessibility of structurally diversified 4-hydroxyquinolinone derivatives remains a key limitation for systematic biological exploration. Despite the broad utility of MCRs in medicinal chemistry, no general and operationally simple method has been reported for the modular assembly of 4
Screwing the helical chirality through terminal peri-functionalization
Beilstein J. Org. Chem. 2026, 22, 205–212, doi:10.3762/bjoc.22.14
- components in organic field effect transistors (OFETs), molecular wires, and chiral conductive materials [19][20][21]. Furthermore, helicenes are widely explored in chiroptical sensing, molecular recognition, and supramolecular self-assembly, enabling the construction of next generation responsive materials
Recent advancements in the synthesis of Veratrum alkaloids
Beilstein J. Org. Chem. 2025, 21, 2657–2693, doi:10.3762/bjoc.21.206
- dense stereochemistry and, thus, have stood long as benchmarks in chemical synthesis. Recently, these steroid alkaloids gained popularity as challenging targets in total synthesis, with a clear shift toward convergent strategies. Not only do these syntheses feature rapid assembly of their challenging
Efficient solid-phase synthesis and structural characterization of segetalins A–H, J and K
Beilstein J. Org. Chem. 2025, 21, 2612–2617, doi:10.3762/bjoc.21.202
- (Scheme 1). Building upon previous work [17][18][19], we focused on optimizing key parameters: resin selection, Fmoc deprotection conditions, coupling reagents for linear assembly, and crucially, the cyclization step. Cost-effectiveness and commercial availability led us to select 2-chlorotrityl chloride
- resin as the solid support, enabling mild cleavage of the partially protected linear peptide precursor [21]. Efficient Fmoc deprotection was achieved using a solution of 1% pyridine and 1% 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) in N,N-dimethylformamide (DMF) [22]. For the assembly of the linear
Recent advances in total synthesis of illisimonin A
Beilstein J. Org. Chem. 2025, 21, 2571–2583, doi:10.3762/bjoc.21.199
- configuration. Kalesse and co-workers accomplished the first asymmetric total synthesis of (−)-illisimonin A based on strategies involving spiro substructure assembly and rearrangement. Consideration of the biosynthetic pathway of illisimonin A inspired Yang and co-workers to develop a bioinspired synthetic
Total syntheses of highly oxidative Ryania diterpenoids facilitated by innovations in synthetic strategies
Beilstein J. Org. Chem. 2025, 21, 2553–2570, doi:10.3762/bjoc.21.198
- function as an engine, consistently pushing the boundaries of the discipline. From the early synthesis of simple molecules to the current precise assembly of complex natural products and functional materials, the iteration of methods and optimization of strategies have always been key to breaking through
- and structurally established [16][17][18]. Structurally, ryanodine (1) and related diterpenoid natural products feature a 6-5-5-5-6 pentacyclic core skeleton containing 11 stereocenters, eight of which are quaternary carbons. A key structural feature is the assembly of a polycyclic cage-like framework
- approach is akin to “taking an elevator”, prioritizing the rapid assembly of the molecular core skeleton before undertaking precise late-stage functionalization. This strategy has proven highly successful for synthesizing complex terpenoids, as exemplified by the Baran group’s 2013 total synthesis of
Synthesis and characterization of a isothiouronium-calix[4]arene derivative: self-assembly and anticancer activity
Beilstein J. Org. Chem. 2025, 21, 2535–2541, doi:10.3762/bjoc.21.195
- potential to load drug molecules in the bioactive nanoassembled structure. Keywords: anticancer agent; calixarene; nanostructure; self-assembly; Introduction Cancer remains one of the leading causes of morbidity and mortality worldwide. Despite significant advancements in chemotherapy, more effective and
- anticancer activity. The synthesis and structural characterization of compound 3 were carried out, and its self-assembly behavior in aqueous medium was investigated using dynamic light scattering (DLS) and electrophoretic light scattering (ELS). The anticancer potential of compound 3 was assessed in human
- functionalization of the calix[4]arene skeleton blocked in cone conformation, as evidenced by the AX system (3.13 and 4.26 ppm) for the bridged CH2 protons. Spontaneous self-assembly Due to the amphiphilic nature, compound 3 could spontaneously self-assemble in aqueous medium. This was confirmed by dynamic light
Assembly strategy for thieno[3,2-b]thiophenes via a disulfide intermediate derived from 3-nitrothiophene-2,5-dicarboxylate
Beilstein J. Org. Chem. 2025, 21, 2489–2497, doi:10.3762/bjoc.21.191
An Fe(II)-catalyzed synthesis of spiro[indoline-3,2'-pyrrolidine] derivatives
Beilstein J. Org. Chem. 2025, 21, 2383–2388, doi:10.3762/bjoc.21.183
- e) [12]. The second category of synthetic methods relies on more accessible, non-pre-functionalized starting materials and stepwise assembly of the spirocyclic core. This strategy enables the synthesis of functionalized 3H-indoles, which can be further elaborated into structurally diverse products
Recent advances in Norrish–Yang cyclization and dicarbonyl photoredox reactions for natural product synthesis
Beilstein J. Org. Chem. 2025, 21, 2315–2333, doi:10.3762/bjoc.21.177
- unprecedented 4,5-spirocyclic B/C ring system and a [4,3,1]propellane F/G/H ring fragment. In 2024, Yang's group achieved the construction of the ABCDE pentacyclic skeleton of phainanoids, leveraging Norrish–Yang cyclization to accomplish the regio- and stereoselective assembly of the rigid, sterically
Pathway economy in cyclization of 1,n-enynes
Beilstein J. Org. Chem. 2025, 21, 2260–2282, doi:10.3762/bjoc.21.173
- substituents serve as critical switches for determining reaction pathway selection. Chemists have developed sophisticated synthetic strategies for programmable assembly of complex small molecular framework by leveraging substituent electronic and steric effects. In 2006, the Shibata group reported a gold
- nitrogen was strategically functionalized with an electron-withdrawing groups (EWGs) and the alkyne of propiolamide was modified with a less bulky substituent. A 6-exo-dig cyclization yielded intermediate 45. Finally, a tandem 6-endo-dig cyclization enabled the successful assembly of the indolo[2,3-a
- nexus for the rational design and optimization of highly effective, selective homogeneous catalytic systems. In 2013, Barriault and co-workers demonstrated that strategic modulation of steric and electronic ligand parameters within gold(I)-catalyzed cyclization pathways enables the selective assembly of
Bioinspired total syntheses of natural products: a personal adventure
Beilstein J. Org. Chem. 2025, 21, 2048–2061, doi:10.3762/bjoc.21.160
- assembly of a complex natural product with a three-dimensional framework in a cascade way. Later, this was regarded as an artificial mimic in laboratory of the biochemical transformations in nature. In the 20th century, Woodward elevated the field of natural product total synthesis to the artistic status
Solar thermal fuels: azobenzene as a cyclic photon–heat transduction platform
Beilstein J. Org. Chem. 2025, 21, 2036–2047, doi:10.3762/bjoc.21.159
- system. Photoisomerization of different types of molecular optical switches. Figure 2 was redrawn from [8]. Nanocarbon-based azobenzene polymer solar thermal fuels: (a) SWCNT templating. Figure 3a is from [43] (T. J. Kucharski et al., “Templated assembly of photoswitches significantly increases the
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