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Search for "synthetic methodologies" in Full Text gives 99 result(s) in Beilstein Journal of Organic Chemistry.
Copper-catalyzed domino cyclization of anilines and cyclobutanone oxime: a scalable and versatile route to spirotetrahydroquinoline derivatives
Beilstein J. Org. Chem. 2025, 21, 749–754, doi:10.3762/bjoc.21.58
- conditions (Scheme 1a) [5][6][7][8]. Consequently, the development of efficient synthetic methodologies for constructing fused THQs is of paramount importance for advancing pharmaceutical research. Conventional synthetic strategies for THQs, which involve the formation of highly strained rings, typically
Formaldehyde surrogates in multicomponent reactions
Beilstein J. Org. Chem. 2025, 21, 564–595, doi:10.3762/bjoc.21.45
- concerns and improved reaction control can be addressed, paving the way for more efficient and sustainable synthetic methodologies. Keywords: cascade reactions; formaldehyde surrogates; green chemistry; heterocycles; multicomponent reactions; Introduction Organic chemistry is a mature discipline that has
Photomechanochemistry: harnessing mechanical forces to enhance photochemical reactions
Beilstein J. Org. Chem. 2025, 21, 458–472, doi:10.3762/bjoc.21.33
- research. Keywords: light-mediated synthesis; mechanochemistry; photomechanochemistry; Introduction Light-mediated synthetic methodologies have significantly transformed contemporary organic chemistry by enabling a broad array of previously unattainable transformations [1]. In fact, the absorption of a
Molecular diversity of the reactions of MBH carbonates of isatins and various nucleophiles
Beilstein J. Org. Chem. 2025, 21, 286–295, doi:10.3762/bjoc.21.21
- synthetic methodologies and in continuation of our aim to develop domino reactions based on MBH carbonates of isatins for efficient construction of diverse polycyclic spiroindolinones [42][43][44][45][46][47][48][49][50][51][52], herein, we wish to report the nucleophilic substitution reactions of various N
Recent advances in electrochemical copper catalysis for modern organic synthesis
Beilstein J. Org. Chem. 2025, 21, 155–178, doi:10.3762/bjoc.21.9
- reactions are essential synthetic methodologies. The discovery of Chan–Lam coupling reactions, which use arylboronic acids and N-nucleophiles, provided a C–N bond-forming protocol using copper catalysis, offering a complementary method to noble transition-metal catalysis [78]. Recently, dual-catalytic
Efficient synthesis of fluorinated triphenylenes with enhanced arene–perfluoroarene interactions in columnar mesophases
Beilstein J. Org. Chem. 2024, 20, 3263–3273, doi:10.3762/bjoc.20.270
- expand this chemistry, enabling access to new π-extended molecular systems that might be challenging to synthesize through conventional synthetic routes. This dual focus highlights the study’s potential to advance both the design of functional materials and the development of innovative synthetic
- methodologies. The mesomorphous properties of these two sets of compounds were investigated by polarized optical microscopy (POM), differential scanning calorimetry (DSC), and small-and wide-angle X-ray scattering (S/WAXS) and compared to related fluorinated and non-fluorinated homologs. The results showed that
Advances in the use of metal-free tetrapyrrolic macrocycles as catalysts
Beilstein J. Org. Chem. 2024, 20, 3085–3112, doi:10.3762/bjoc.20.257
- second-sphere interactions with a multipoint hydrogen-bonding pattern enhance CO2 reduction in organic solvents, improving stability, facilitating proton transfer, reducing energy barriers, and increasing selectivity [20]. Apart from advances in synthetic methodologies [2][21][22][23], the exploration of
- the examples mentioned above indicate that calix[4]pyrroles can be used as organocatalysts. Despite major advancements in synthetic methodologies to synthesize functionalized calix[4]pyrrole macrocycles, not much progress has been done in this area in recent years. One of the major challenges of using
The Groebke–Blackburn–Bienaymé reaction in its maturity: innovation and improvements since its 21st birthday (2019–2023)
Beilstein J. Org. Chem. 2024, 20, 1839–1879, doi:10.3762/bjoc.20.162
- active ones by DNA sequencing. Great challenges, however, characterize the synthetic methodologies, since the chemistry must display a broad scope, be compatible with water and operationally simple, and preserve the genetic information (i.e., no harsh conditions, strongly acidic pHs, no oxidants or Lewis
Syntheses and medicinal chemistry of spiro heterocyclic steroids
Beilstein J. Org. Chem. 2024, 20, 1713–1745, doi:10.3762/bjoc.20.152
- is compelling evidence that incorporating a heterocyclic moiety into a steroid can alter its pharmacological and pharmacokinetic properties, driving intense interest in the synthesis of such hybrids among research groups. In this review, we present an overview of recent synthetic methodologies
Chemo-enzymatic total synthesis: current approaches toward the integration of chemical and enzymatic transformations
Beilstein J. Org. Chem. 2024, 20, 1693–1712, doi:10.3762/bjoc.20.151
- substrates of SorbC [43]. Almost concurrently, Narayan and co-workers substantially expanded the application scope of synthetic methodologies by utilizing the FAD-dependent monooxygenase TropB, AzaH, and SorbC to catalyze oxidative dearomatization [38][39]. Through extensive exploration of substrate
- classification, along with parallel discussions of the original biosynthetic pathways, helps organize the current state of the art and offers a comprehensive overview of how synthetic methodologies leverage the natural biosynthetic pathways. The development and optimization of chemo-enzymatic synthetic processes
Bismuth(III) triflate: an economical and environmentally friendly catalyst for the Nazarov reaction
Beilstein J. Org. Chem. 2024, 20, 1167–1178, doi:10.3762/bjoc.20.99
- ; indanones; Nazarov reaction; Introduction Natural products are the source of inspiration for several research groups that develop new synthetic methodologies. The chemistry of five-membered rings plays an important role in organic chemistry, both because of the wide occurrence in nature [1][2][3][4][5][6
Entry to new spiroheterocycles via tandem Rh(II)-catalyzed O–H insertion/base-promoted cyclization involving diazoarylidene succinimides
Beilstein J. Org. Chem. 2024, 20, 561–569, doi:10.3762/bjoc.20.48
- modern drug design [1][2]. They are known to promote higher success rates, when targeting three-dimensional protein molecules [3][4]. Furthermore, a wide variety of spirocyclic fragments can be spotted in natural products [5]. The aspects mentioned unveil the development of synthetic methodologies
1-Butyl-3-methylimidazolium tetrafluoroborate as suitable solvent for BF3: the case of alkyne hydration. Chemistry vs electrochemistry
Beilstein J. Org. Chem. 2023, 19, 1966–1981, doi:10.3762/bjoc.19.147
- -heterocyclic carbenes (NHCs), extensively studied as organocatalysts as well as ligands for transition-metal-promoted synthetic methodologies [97][98][99]. Under anodic oxidation, the electrogeneration of boron trifluoride (BF3) from tetrafluoroborate ILs occurs [100][101]. Moreover, we have recently
Construction of diazepine-containing spiroindolines via annulation reaction of α-halogenated N-acylhydrazones and isatin-derived MBH carbonates
Beilstein J. Org. Chem. 2023, 19, 1923–1932, doi:10.3762/bjoc.19.143
- alternative synthetic methodologies for functionalized 1,2-diazepines has drawn extensive attention [14][15][16][17][18][19][20][21]. One of the most attractive strategies to synthesize the 1,2-diazepine motif represents the [4 + 3] cycloaddition reaction between activated azoalkenes and 1,3-dipolarophiles
- [22][23][24][25][26][27]. In addition, spirooxindole is also a privileged structural scaffold, which has been recognized as key structural unit in many bioactive natural products and pharmaceuticals with broad biological activities [28][29][30]. The development of elegant synthetic methodologies for
Trifluoromethylated hydrazones and acylhydrazones as potent nitrogen-containing fluorinated building blocks
Beilstein J. Org. Chem. 2023, 19, 1741–1754, doi:10.3762/bjoc.19.127
- lipophilicity and metabolic stability compared to nonfluorinated compounds [1][2][3][4][5]. At present, about 300 drug molecules and over 400 pesticides on the market contain at least one fluorine atom [6][7]. Therefore, the development of novel and effective synthetic methodologies for the synthesis of
Synthesis of ether lipids: natural compounds and analogues
Beilstein J. Org. Chem. 2023, 19, 1299–1369, doi:10.3762/bjoc.19.96
Selective construction of dispiro[indoline-3,2'-quinoline-3',3''-indoline] and dispiro[indoline-3,2'-pyrrole-3',3''-indoline] via three-component reaction
Beilstein J. Org. Chem. 2023, 19, 1234–1242, doi:10.3762/bjoc.19.91
- in many bioactive natural and synthetic compounds [1][2][3]. It is known that many spirooxindole derivatives show important biological activities [4][5][6]. On the other hand, a wide range of differently substituted spirooxindoles exist [7][8][9]. Therefore, the development of efficient synthetic
- methodologies for diverse spirooxindoles have become one of the hottest research fields in organic and pharmaceutical chemistry [10][11]. In order to synthesize diverse spirooxindole derivatives, commercially available isatins and easily obtainable 3-methyleneoxindolines were the most employed building blocks
The unique reactivity of 5,6-unsubstituted 1,4-dihydropyridine in the Huisgen 1,4-diploar cycloaddition and formal [2 + 2] cycloaddition
Beilstein J. Org. Chem. 2023, 19, 982–990, doi:10.3762/bjoc.19.73
- behaved as an activated electron-rich dienophile. Inspired by these elegant synthetic methodologies and in continuation of our aim to develop well-known Huisgen 1,4-dipoles for the construction of diverse nitrogen-containing heterocyclic compounds [45][46][47][48][49][50][51][52][53][54][55][56][57][58
- unprecedented synthetic reactivity of the electron-deficient alkynes, but also provides efficient synthetic methodologies for complex nitrogen-containing heterocycles. The potential application of this reaction in organic synthesis and medicinal chemistry might be significant. Experimental General procedure for
Light-responsive rotaxane-based materials: inducing motion in the solid state
Beilstein J. Org. Chem. 2023, 19, 873–880, doi:10.3762/bjoc.19.64
- light-responsive intertwined materials and the industrial scale-up production usually hindered by the low yield of the interlocked molecules. Thus, future research efforts should be focused on the development of novel synthetic methodologies to access to such interlocked architecture, as well as the use
Facile access to 3-sulfonylquinolines via Knoevenagel condensation/aza-Wittig reaction cascade involving ortho-azidobenzaldehydes and β-ketosulfonamides and sulfones
Beilstein J. Org. Chem. 2023, 19, 800–807, doi:10.3762/bjoc.19.60
- through a range of synthetic methodologies suggested recently. Cyclization strategies [35][36][37][38][39][40][41][42][43][44][45] as well as cycloaddition/cyclocondensation techniques [46][47][48][49][50][51] represent those with hetero-ring construction. Alternative approaches rely on a peripheral
Total synthesis: an enabling science
Beilstein J. Org. Chem. 2023, 19, 474–476, doi:10.3762/bjoc.19.36
- Bastien Nay Laboratoire de Synthèse Organique, École Polytechnique, CNRS, ENSTA, Institut Polytechnique de Paris, 91128 Palaiseau, France 10.3762/bjoc.19.36 Keywords: chemical complexity; natural products; synthetic methodologies; total synthesis; Total synthesis is a topic strongly related to
- enabling science. Total synthesis is the science of constructing molecules from simple starting materials. It often deals with complex molecular architectures that require a thorough retrosynthetic problem-solving analysis [7]. Total synthesis and the discovery of new synthetic methodologies have always
1,4-Dithianes: attractive C2-building blocks for the synthesis of complex molecular architectures
Beilstein J. Org. Chem. 2023, 19, 115–132, doi:10.3762/bjoc.19.12
- , should open up many more possibilities. Moreover, as the synthetic access to these sulfur-based heterocycles is now more straightforward, the importance of 1,4-dithianes and related heterocycles in new synthetic methodologies can be expected. An area where these C2-synthons have so far been less
Redox-active molecules as organocatalysts for selective oxidative transformations – an unperceived organocatalysis field
Beilstein J. Org. Chem. 2022, 18, 1672–1695, doi:10.3762/bjoc.18.179
- stoichiometric oxidants. The development of organic chemistry is strongly affected by rising “green” demands to synthetic methodologies, including reduction of waste formation, low trace-metal content in drug compounds, high energy-efficiency and selectivity of processes. In the last decade researchers proposed
Efficient synthesis of aziridinecyclooctanediol and 3-aminocyclooctanetriol
Beilstein J. Org. Chem. 2022, 18, 1539–1543, doi:10.3762/bjoc.18.163
- antibiotic activities. Therefore, synthetic methodologies for the preparation of the aziridinyl system have attracted attention in recent decades. Opening of the aziridine ring by using different nucleophiles gives the corresponding amino alcohols, amino esters, azido amines, amines, and other derivatives [9
Synthesis of α-(perfluoroalkylsulfonyl)propiophenones: a new set of reagents for the light-mediated perfluoroalkylation of aromatics
Beilstein J. Org. Chem. 2022, 18, 788–795, doi:10.3762/bjoc.18.79
- character – have been harnessed in a plethora of applications in modern life: Teflon in non-stick pans, fire-fighting foams, stain-resistant and weatherproof fabrics, etching of circuit boards, and even imaging agents [1]. Given their importance, multiple synthetic methodologies for the introduction of long
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