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Search for "one-pot" in Full Text gives 863 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.
Modern synthetic pathways towards eribulin and its subunits
Beilstein J. Org. Chem. 2026, 22, 495–526, doi:10.3762/bjoc.22.37
- dicarbonyl via Swern oxidation, and finally olefinated via Wittig reaction. Hence, by the use of one-pot Au(I)-catalyzed cyclization/Kishi reduction for the assembly of the tetrahydropyran and cross metathesis/Sharpless dihydroxylation/etherification for the tetrahydrofuran motifs, this pathway describes a
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
- -containing five-membered rings with iridium complexes and examined the influence of different alcohol protecting groups on the monoalkyne substrates. The reaction proceeded in generally high yields (>70%) with satisfactory enantioselectivity. Building on this work, Shibata and Tsuchikama developed a one-pot
Dialkylaminoalkylation of β-ketosulfones via ring-opening of 3-sulfonylpyrrolidines
Beilstein J. Org. Chem. 2026, 22, 383–389, doi:10.3762/bjoc.22.26
- promote Hofmann elimination. To enhance the leaving ability of the nitrogen atom we prepared ammonium salts 3 of the obtained pyrrolidines via treatment with alkyl halides. Since the preparation of quaternary ammonium salts of pyrrolidines is straightforward, we employed a one-pot method for its synthesis
- pyrrolidines as sacrificial framework and two domino processes used for assembling of the pyrrolidine ring and for the ring-cleavage of it. Thus, one-pot pyrrolidination of β-ketosulfones and alkylation combined with the subsequent debenzoylative ring-cleavage allows for wide range of the incorporated reagents
Electrosynthetic access to unsymmetrical oxaza[8]helicenes with high chiral stability and strong circularly polarized luminescence (CPL)
Beilstein J. Org. Chem. 2026, 22, 372–382, doi:10.3762/bjoc.22.25
- Supporting Information File 1), we developed a one-pot electrochemical annulation between 3 and β-naphthol derivative 4. Using n-Bu4NPF6 as the electrolyte in CH2Cl2 at room temperature, this protocol furnished oxaza[8]helicenes 5 in good-to-moderate yields with >75% Faradaic efficiency, and no homo-coupling
Synthesis of tricyclic fused pyrrolidine nitroxides from 2-alkynylpyrrolidine-1-oxyls
Beilstein J. Org. Chem. 2026, 22, 344–351, doi:10.3762/bjoc.22.22
- Huisgen cycloaddition or via one-pot Michael addition–cyclocondensation reaction with hydrazine with subsequent intramolecular alkylation of the resulting pyrazoles. Results and Discussion Synthesis We have earlier reported on the synthesis of 2-alkynylpyrrolidine-1-oxyls 2a–c via addition of the
Spirobarbiturates with a pyrrolizidine moiety: synthesis, structure and biological evaluation
Beilstein J. Org. Chem. 2026, 22, 274–288, doi:10.3762/bjoc.22.20
- 10.3762/bjoc.22.20 Abstract Polycyclic spirobarbiturates containing a pyrrolizidine moiety were synthesized via a one-pot three-component 1,3-dipolar cycloaddition reaction of alloxan, ʟ-proline and N-substituted maleimides. The reaction stereoselectivity was found to depend on the nature of substituents
- depolymerization that continuously occur in cells. Conclusion We have developed a novel one-pot three-component method for the synthesis of pyrrolizidine-containing spirobarbiturates via 1,3-dipolar cycloaddition reactions. The study revealed that maleimide derivatives with -H, -Me, -Ph, p-Tol, or 4-NO2С6H4
- . Synthesis of racemic spirobarbiturates 4a–p via one-pot three-component reaction of alloxan (1), ʟ-proline (2) and N-substituted maleimides 3. A plausible mechanism of spirobarbiturate formation from alloxan (1), ʟ-proline (2), and N-substituted maleimides 3a–p. Supporting Information Supporting
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
- acids followed by sequential Michael-type addition and subsequent cascade transformations. This versatile one-pot protocol delivers structurally diverse open-chain 3-arylpropanoate esters in moderate to good yields (46–69%), while cyclic pyranoquinolinones are formed under kinetically controlled
- , 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
- quantitatively. Although the two-step sequence generally performed well, isolation of malonamides 1a–c was associated with significant material loss, impacting the overall yield. To address this, a one-pot synthesis directly from anilines was developed, avoiding isolation of intermediates. After approximately 4
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
- difficult for the substrate to coordinate with the metal catalyst. In 2021, Glorius and co-workers reported an enantio- and diastereoselective complete hydrogenation of substituted benzofurans 65 in a one-pot cascade reaction (Scheme 8) [62]. This method facilitates the controlled installation of up to six
- benzylic alcohol with TFA/Et₃SiH afforded pyridine 95, which underwent a one-pot sequence of indole protection, methylation, and hydrogenation to furnish tetrahydropyridine 96. In contrast to Vollhardt’s synthesis, the unsaturation was misaligned with that of the natural product, most likely arising from
- between 179 and the dicarbonyl compound, followed by in-situ oxidation of the resulting intermediate 180 to afford compound 181 in a one-pot sequence. At this step, the key challenge was to obtain (−)-finerenone with high enantioselectivity through asymmetric hydrogenation of intermediate 181 (Scheme 25
Advances in Zr-mediated radical transformations and applications to total synthesis
Beilstein J. Org. Chem. 2026, 22, 71–87, doi:10.3762/bjoc.22.3
- conditions required. As an alternative, dithiane-based ketone synthesis has long been used, but it suffers from drawbacks in terms of step economy [10][11]. To address these limitations, the authors developed a radical-based one-pot ketone synthesis that proceeds under mild conditions. When thioester 11 and
- synthesis of homohalichondrin B (58). This synthetic strategy proved broadly applicable to multiple members of the halichondrin family, enabling the efficient synthesis of nine natural products: halichondrins A–C, norhalichondrins A–C, and homohalichondrins A–C. The Zr/Ni-mediated one-pot ketone synthesis
- background of zirconium and its physical properties. Image depicted in the background of Figure 1 was purchased from iStock.com/Just_Super. This content is not subject to CC BY 4.0. Zr-mediated radical cyclization. Ni/Zr-mediated one-pot ketone synthesis. Zirconocene-catalyzed alkylative dimerization of 2
Synthesis and applications of alkenyl chlorides (vinyl chlorides): a review
Beilstein J. Org. Chem. 2026, 22, 1–63, doi:10.3762/bjoc.22.1
- , only tertiary aliphatic substrates were examined, generating non-stabilized carbocations. While the transformations proceeded cleanly, yields were generally low and the scope was restricted to non-functionalized arylalkynes. A one-pot procedure for the in situ generation of benzylic cations from
One-pot synthesis of ethylmaltol from maltol
Beilstein J. Org. Chem. 2025, 21, 2755–2760, doi:10.3762/bjoc.21.212
- via methylation of a dianionic intermediate, proved unsuitable due to competing overalkylation and the necessity of sub-zero temperatures. In contrast, a transient protecting group approach enabled selective methylation under mild conditions. This culminated in a scalable, operationally simple one-pot
- one-pot conversion of alcohol 5 to ethylmaltol (1) and various patents have focused on this transformation [14][15][16][17][18][19]. While maltol (2) can be obtained through analogous sequences from kojic acid (3) [4][20][21] or furfural (4) [7][9][11][12][13], it is naturally occurring in the leaves
- ), selective methylation of maltol (2) would represent the most direct access to ethylmaltol (1). Herein, we disclose an operationally simple, one-pot methylation procedure to access ethylmaltol (1) from maltol (2, Scheme 1c). Results and Discussion Inspired by the selective γ-alkylation of dianions of β-keto
Recent advancements in the synthesis of Veratrum alkaloids
Beilstein J. Org. Chem. 2025, 21, 2657–2693, doi:10.3762/bjoc.21.206
- , color-coding each transformation in this one-pot procedure. Cascade reactions, as well as reactions, where a single set of reaction conditions and reagents transform two or more groups simultaneously (e.g., global deprotections) and reactions, that occur upon work-up, are still regarded as one step and
- formation and reductive coupling with an aldehyde made accessible β-amino alcohol 60 over two steps. A cascade reaction occurred upon treatment with HCl in acetone followed by treatment with KOH. Indeed, a tandem 5-exo-trig cyclization, sulfinyl removal, and lactamization occurred in one-pot. Finally
- in C14–C15 via a Horner–Wadsworth–Emmons (HWE) reaction. Interestingly, the left-hand fragment is synthesized in an unusual thermal Eschenmoser fragmentation, the product being directly conjoined in a one-pot fashion. First, commercially available (S)-3-methylpiperidine (74) was N-protected and
Synthesis of new tetra- and pentacyclic, methylenedioxy- and ethylenedioxy-substituted derivatives of the dibenzo[c,f][1,2]thiazepine ring system
Beilstein J. Org. Chem. 2025, 21, 2645–2656, doi:10.3762/bjoc.21.205
- followed by basic hydrolysis afforded carboxylic acids 14 and 15. Ring closure of the latter compounds to tetracyclic derivatives 6 and 7 was carried out in one pot by SnCl4-catalyzed Friedel–Crafts cyclization of the acid chlorides obtained via reaction of 14 and 15 with phosphorus pentachloride. In the
Visible-light-driven NHC and organophotoredox dual catalysis for the synthesis of carbonyl compounds
Beilstein J. Org. Chem. 2025, 21, 2584–2603, doi:10.3762/bjoc.21.200
- valuable approach for the α-functionalization of ketones using visible-light irradiation under mild reaction conditions. In a one-pot procedure, the reaction was carried out between alkenes 28 and coupling partner 29 in the presence of NHC (30 mol %) and a photocatalyst (5 mol %). Under these conditions
Recent advances in total synthesis of illisimonin A
Beilstein J. Org. Chem. 2025, 21, 2571–2583, doi:10.3762/bjoc.21.199
- , which was subsequently subjected to a one-pot desilylation to afford 24. Reduction of both the ester and ketone functionalities in 24, followed by selective protection of the primary alcohol and re-oxidation of the secondary alcohol to ketone, furnished compound 25 in three steps. The ketone in 25 was
- introduce another side chain, affording a diene intermediate. A subsequent ring-closing metathesis (RCM) reaction formed the cyclopentene ring, and one pot protection of both carbonyl groups with ethylene glycol provided bis-ketal 55. Notably, due to steric hindrance, only one carbonyl group could be
- protected prior to the RCM step. Oxidative cleavage of the cyclopentene followed by Pinnick oxidation of the resulting aldehyde to the carboxylic acid and esterification yielded ketoester 56. Dieckmann condensation of 56, esterification of the resulting enolate with 57, and subsequent one-pot partial
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
- conditions induces the first intramolecular reductive cyclization, affording hemiacetal 27. This intermediate is then transformed via a one-pot sequence involving epoxidation, fragmentation, and re-epoxidation to give epoxide 29. A second intramolecular reductive cyclization of 29 under Li/NH3 forms the
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
- -dicarboxylates by its one-pot reduction–alkylation using NaBH4 in DMF followed by an alkylating agent. Base-promoted cyclization of electron-deficient 3-alkylthio derivatives furnished 2-aryl-, 2-aroyl-, and 2-cyano-substituted thieno[3,2-b]thiophenes, bearing a 3-hydroxy group. This protocol broadens access to
- -3-yl lithium derivative, followed by electrophilic trapping of the thiolate and base-induced cyclization to afford the 3-hydroxy-TT [25]. Route II is represented by the single example of a one-pot reaction of 2-methylquinoline and 3-bromothiophene-2-carbaldehyde in the presence of elemental S and
- of the S–S bond in disulfide 3 followed by in situ alkylation was investigated for the one-pot synthesis of 3-alkylthio-substituted thiophene-2,5-dicarboxylates. We first focused our efforts on optimizing the conditions of this two-step process to determine suitable reducing agents and solvents
Ex-situ generation of gaseous nitriles in two-chamber glassware for facile haloacetimidate synthesis
Beilstein J. Org. Chem. 2025, 21, 2465–2469, doi:10.3762/bjoc.21.188
- sufficient to be used in a subsequent reaction, hence demonstrating the advantage of using a two-chamber system compared to a one-pot setup, where excess reagents would be present in the crude. As mentioned in the introduction, trifluoroacetonitrile is often used to synthesize a variety of heterocycles via
Transformation of the cyclohexane ring to the cyclopentane fragment of biologically active compounds
Beilstein J. Org. Chem. 2025, 21, 2416–2446, doi:10.3762/bjoc.21.185
- completed by converting the exocyclic methyl ester 144 to an aldehyde145 using a one-pot DIBAL-H/Dess–Martin procedure followed by the removal of TMS protecting group using a stoichiometric Wilkinson’s catalyst (Scheme 25). The authors noted that, in the final stages of reduction and oxidation, yields were
Comparative analysis of complanadine A total syntheses
Beilstein J. Org. Chem. 2025, 21, 2334–2344, doi:10.3762/bjoc.21.178
- in four steps. Subsequent conjugate addition of the lithium anion of TMS-acetonitrile to 15, followed by careful one-pot protonation of the resulting enolate with ethyl salicylate and TMS removal with CsF, gave 16 bearing three properly arranged substituents. Grignard 1,2-addition to ketone 16
- . to forge the C2–C3’ bipyridyl linkage and produce 56 in good yield [30]. From 56, a one-pot Cbz removal and pyridine N-oxide reduction completed their total synthesis of complanadine A. In addition, 56 also served as a key intermediate for their synthesis of complanadine B, which was achieved via a
- TMSN3 recently developed by Xu and co-workers [34]. Mukaiyama conjugate addition between 60 and 61 promoted by Tf2NH followed by a one-pot enol ether hydrolysis gave 62 as a mixture of inconsequential stereoisomers. Subsequent oxidative cleavage of the terminal olefin of 62 using ozonolysis followed by
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
- by the Yang group [22]. Installation of the hydroxymethyl group in 4 was achieved through sequential formylation and reduction. Compound 4 then underwent a one-pot, substrate-controlled diastereoselective Johnson−Claisen rearrangement/acetylation to install ester 5. Treating 5 with m-CPBA (meta
- delivered 68. A one-pot desilylation/oxidation of 67 produced an aldehyde, which was subject to selective nucleophilic addition in the presence of a ketone, allowing for access to the furan precursor 68 [37]. Oxidation–cyclization–aromatization of 68 with Dess–Martin periodinane (DMP) constructed the
- – was prepared from (+)-pulegone (77) through a six-step manipulation involving epoxidation, epoxide opening with sodium thiophenolate and subsequent concomitant retro-aldol, sulfoxidation, a one pot α-alkylation with acrylonitrile proceeding to thermal syn-elimination of phenylsulfenic acid, ketone
Halogenated butyrolactones from the biomass-derived synthon levoglucosenone
Beilstein J. Org. Chem. 2025, 21, 2297–2301, doi:10.3762/bjoc.21.175
- oxymethylene bridge in the 2D NOESY NMR spectrum. Given the instability of fluoro-ketone 13, a one-pot procedure was developed in which the reaction mixture containing 13 was subjected to the Baeyer–Villiger oxidation with H2O2 giving the fluorinated and stable lactone 14, which is the expected kinetic product
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
- a Pd-catalyzed three-step sequence to access a wide range of non-symmetric azobenzenes (Figure 1b, bottom) [43][44]. Inspired by these approaches and building on recent advances in the dehydrogenation of 1,2-diarylhydrazines to azobenzenes [45][46][47][48][49][50], we developed a one-pot strategy
- azobenzenes; b) previous Pd-catalyzed methods for the synthesis of non-symmetric azobenzenes; c) this work: Pd-catalyzed dehydrogenative C–N coupling of arylhydrazine. a) Proposed catalytic cycle for the one-pot palladium-catalyzed dehydrogenative C–N coupling for the synthesis of azobenzene from
Thiadiazino-indole, thiadiazino-carbazole and benzothiadiazino-carbazole dioxides: synthesis, physicochemical and early ADME characterization of representatives of new tri-, tetra- and pentacyclic ring systems and their intermediates
Beilstein J. Org. Chem. 2025, 21, 2220–2233, doi:10.3762/bjoc.21.169
- synthesis [18][19][20][21]. Sudhakara et al. described the advantages of using bismuth nitrate as catalyst in the synthesis of hydrazones and in the one-pot Fischer synthesis of indoles from ketones and hydrazines [22][23]. Adopting this method, hydrazone intermediates 7a–j were obtained by treatment of
- conditions. Finally, we were able to achieve the Fischer cyclization of compounds 7a–j by using p-toluenesulfonic acid monohydrate as catalyst in boiling toluene (method A, step 2) [26][27]. On the other hand, the one-pot synthesis of target compounds 3a–j starting from hydrazino derivatives 5a,b was
- derivatives 10a,b exhibiting an extended aromatic ring system were isolated instead of the expected primarily formed congeners 11a,b, due to in situ oxidation of the C–C bond. Alternatively, when the one-pot method (method B, bismuth nitrate pentahydrate + PPA, MeOH, closed vial, 110 °C) was applied for the
Synthesis of triazolo- and tetrazolo-fused 1,4-benzodiazepines via one-pot Ugi–azide and Cu-free click reactions
Beilstein J. Org. Chem. 2025, 21, 2202–2210, doi:10.3762/bjoc.21.167
- /bjoc.21.167 Abstract A one-pot Ugi–azide reaction followed by intramolecular Cu-free azide–alkyne cycloaddition generates a polycyclic scaffold 7 bearing polycyclic triazole, tetrazole, and benzodiazepine rings. This method could be extended for obtaining a more complicated scaffold 8 containing a
- piperazinone ring. Keywords: benzodiazepine; click reaction; multicomponent reaction; one-pot; piperazinone; polycyclic; triazole; tetrazole; Ugi–azide reaction; Introduction Triazole, tetrazole, and benzodiazepine are privileged heterocyclic rings commonly found in drug molecules and functional materials [1
- ]. We herein propose a one-pot synthesis involving an Ugi–azide 4-component (4-CR) reaction followed by lactamization and azide–alkyne cycloaddition for assembling triazole-fused and tetrazole-tethered 1,4-benzodiazepines 7 and triazole-, tetrazole-, and piperazinone-fused 1,4-benzodiazepines 8 (Scheme
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