Rapid access to the core of malayamycin A by intramolecular dipolar cycloaddition

• Yilin Liu,
• Yuchen Yang,
• Chen Yang,
• Sha-Hua Huang,
• Jian Jin and
• Ran Hong

Beilstein J. Org. Chem. 2025, 21, 2542–2547, doi:10.3762/bjoc.21.196

• development of potent fungicides. Keywords: dipolar cycloaddition; elimination; fungicide; nucleoside; oxazoline; Introduction Modern agriculture relies on various effective fungicides to combat crop diseases for achieving significant gains [1]. However, the long-term and widespread use of chemicals and

• to inhibit the sporulation of Stagonospora nodorum (Berk) Castell and Germano that were identified as the culprit of wheat glume blotch disease [5]. Furthermore, malayamycin functions as a broad-spectrum fungicide with an unusually higher potency in planta than in vitro, suggesting that its mode of

• action may not be consistent with those of known fungicide classes. This encouraging characteristic indicates its potential to overcome resistance to other fungicides [6][7][8]. Structurally, malayamycin A belongs to a class of modified nucleosides that mimic UDP (uridine 5′-diphosphate)-linked

C2 to C6 biobased carbonyl platforms for fine chemistry

• Jingjing Jiang,
• Muhammad Noman Haider Tariq,
• Florence Popowycz,
• Yanlong Gu and
• Yves Queneau

Beilstein J. Org. Chem. 2025, 21, 2103–2172, doi:10.3762/bjoc.21.165

• -hydroxypropan-2-one with acylacetonitrile towards furan derivatives using a Sc(OTf)3 catalyst. C2-based bifunctional acetals, such as glycolaldehyde diethyl acetal, α-bromoacetaldehyde acetal, and 1,4-dithiane-2,5-diol also take part in the reaction as counterpart reagents. The well-known fungicide fenfuram was

Research progress on calixarene/pillararene-based controlled drug release systems

• Liu-Huan Yi,
• Jian Qin,
• Si-Ran Lu,
• Liu-Pan Yang,
• Li-Li Wang and
• Huan Yao

Beilstein J. Org. Chem. 2025, 21, 1757–1785, doi:10.3762/bjoc.21.139

New triazinephosphonate dopants for Nafion proton exchange membranes (PEM)

• Fátima C. Teixeira,
• António P. S. Teixeira and
• C. M. Rangel

Beilstein J. Org. Chem. 2024, 20, 1623–1634, doi:10.3762/bjoc.20.145

• -triazine isomers [30]. There have been reported several and diverse applications to a large number of compounds with a triazine moiety, ranging from biological applications [31][32][33][34], such as fungicide, herbicide, antiviral, antimicrobial, antitumor, to their use in organic synthesis, including

(Bio)isosteres of ortho- and meta-substituted benzenes

• H. Erik Diepers and
• Johannes C. L. Walker

Beilstein J. Org. Chem. 2024, 20, 859–890, doi:10.3762/bjoc.20.78

• fungicide bixafen and its 1,2-BCH-based bioisostere, as reported in the same publication (not shown). 1,5-Disubstituted bicyclo[2.1.1]hexanes The isomeric 1,5-disubstituted bicyclo[2.1.1]hexanes (1,5-BCHs) have also been suggested as ortho-benzene isosteres [42]. Exit vector analysis reveals that the

• -substituted endo-1,5-BCHs (±)-57a–e. Substrate modification was also possible, with oxidative transformation of a bridgehead furan leading to 1,5-BCH acid (±)-60 and pyridine reduction to secondary amine (±)-61 (Scheme 5B) [42]. Furthermore, 1,5-BCH (±)-64 was synthesised as a bioisostere of the fungicide

Synthesis of 2,2-difluoro-1,3-diketone and 2,2-difluoro-1,3-ketoester derivatives using fluorine gas

• Alexander S. Hampton,
• David R. W. Hodgson,
• Graham McDougald,
• Linhua Wang and
• Graham Sandford

Beilstein J. Org. Chem. 2024, 20, 460–469, doi:10.3762/bjoc.20.41

• significant pharmaceuticals [lubiprostone (constipation), maraviroc (HIV), tafluproct (anti-inflamatory), ledipasvir (hepatitis-C)] and agrochemicals [isopyrazam (fungicide), riodipine (calcium channel blocker), primisulfuron-methyl (pesticide)] owe their enhanced bioactivity, in part, to the presence of

On drug discovery against infectious diseases and academic medicinal chemistry contributions

• Yves L. Janin

Beilstein J. Org. Chem. 2022, 18, 1355–1378, doi:10.3762/bjoc.18.141

• -bearing substances, endowed with an antibacterial effect [58]. However, this compound was originally patented for a fungicide effect [59] and then found to also inhibit mammalian c-Jun N-terminal kinase [60]. Unsurprisingly, it was also reported in 2022 as a covalent inhibitor for the SARS-CoV-2 main

On the application of 3d metals for C–H activation toward bioactive compounds: The key step for the synthesis of silver bullets

• Renato L. Carvalho,
• Amanda S. de Miranda,
• Mateus P. Nunes,
• Roberto S. Gomes,
• Guilherme A. M. Jardim and
• Eufrânio N. da Silva Júnior

Beilstein J. Org. Chem. 2021, 17, 1849–1938, doi:10.3762/bjoc.17.126

5-Aminopyrazole as precursor in design and synthesis of fused pyrazoloazines

• Ranjana Aggarwal and
• Suresh Kumar

Beilstein J. Org. Chem. 2018, 14, 203–242, doi:10.3762/bjoc.14.15

• ], protein kinase inhibitors [32], antiallergic [33], antioxidant [34] and as fungicide [35]. Also, the pyrazolo[3,4-b]pyridine ring system is a key structure in drug discovery and has become the main component in many medicinally important compounds. The large number of synthetic routes to pyrazolo[3,4-b

1,3-Dibromo-5,5-dimethylhydantoin as promoter for glycosylations using thioglycosides

• Fei-Fei Xu,
• Claney L. Pereira and
• Peter H. Seeberger

Beilstein J. Org. Chem. 2017, 13, 1994–1998, doi:10.3762/bjoc.13.195

• , including dichloromethane, is sold under the trade name Brom-55 and used as swimming pool sanitizer, as industrial brominating agent for ethylene propylene diene monomer rubber to improve ozone resistance, as additive in plastics to promote photodegradation and as a fungicide to preserve fresh fruits [27

Continuous-flow synthesis of primary amines: Metal-free reduction of aliphatic and aromatic nitro derivatives with trichlorosilane

• Riccardo Porta,
• Alessandra Puglisi,
• Giacomo Colombo,
• Sergio Rossi and
• Maurizio Benaglia

Beilstein J. Org. Chem. 2016, 12, 2614–2619, doi:10.3762/bjoc.12.257

• molecules of pharmaceutical interest. The reduction of nitro compound 3 afforded 2-(4'-chlorophenyl)aniline (4), the direct precursor of the fungicide boscalid (Scheme 4). Under the best reaction conditions in a 5 mL PTFE reactor (flow rate 0.1 mL/min, 50 min residence time), the desired amine 4 was

Natural products from microbes associated with insects

• Christine Beemelmanns,
• Huijuan Guo,
• Maja Rischer and
• Michael Poulsen

Beilstein J. Org. Chem. 2016, 12, 314–327, doi:10.3762/bjoc.12.34

• . Using symbiont pairing bioassays and chemical analysis one of the major isolates Streptomyces thermosacchari was shown to produce the fungicide mycangimycin (12), which inhibits the growth of the antagonist O. minus. Mycangimycin is an unusual carboxylic acid derivative with an endoperoxide unit and a

Copper-catalyzed intermolecular oxyamination of olefins using carboxylic acids and O-benzoylhydroxylamines

• Brett N. Hemric and
• Qiu Wang

Beilstein J. Org. Chem. 2016, 12, 22–28, doi:10.3762/bjoc.12.4

• -adrenergic receptor agonist [3]; lumefantrine, an antimalarial drug [4]; ifenprodil, an N-methyl-D-aspartate (NMDA) antagonist [5]; and tebuconazole, a commercial fungicide [6]. With the importance of 1,2-oxyamino motifs as privileged pharmacophores, the development of facile and efficient access to this

Radical-mediated dehydrative preparation of cyclic imides using (NH₄)₂S₂O₈–DMSO: application to the synthesis of vernakalant

• Dnyaneshwar N. Garad,
• Subhash D. Tanpure and
• Santosh B. Mhaske

Beilstein J. Org. Chem. 2015, 11, 1008–1016, doi:10.3762/bjoc.11.113

• ), captan (fungicide), flumipropyn (herbicide), flumioxazin (herbicide), procymidone (pesticide) and cinidon-ethyl (herbicide) [18][19]. Imides are the backbones of several commercially available high-performance polymers [20][21] and many other advanced materials [22][23][24][25]. The most commonly used

• excellent yield (Table 2, entries 11 and 12). Interestingly, the N-phenyl analogue of Captan, a commercially used fungicide could be synthesized in excellent yield (Table 2, entry 12) [18][19]. The reaction of aromatic amines with unsaturated anhydrides to form maleimides was investigated (Table 3). Aniline

Encapsulation of biocides by cyclodextrins: toward synergistic effects against pathogens

• Véronique Nardello-Rataj and
• Loïc Leclercq

Beilstein J. Org. Chem. 2014, 10, 2603–2622, doi:10.3762/bjoc.10.273

• solubility. Carbendazim is a widely used systemic fungicide against different fungi affecting plants [38][39]. Its mechanism is linked to its antimitotic properties that inhibit the bacterial growth [40]. Due to its poor water-solubility, its application becomes a major constraining factor. In 1996, Schmidt

• morphologies, structures and colors of colonies. For higher dosage, a clear decrease in the diameter of the colonies is also reported. In contrast, the use of the biocide alone has no impact on the culture medium in the same range of concentrations. Moreover, this carbamate, which is a systemic fungicide, has

Continuous flow nitration in miniaturized devices

• Amol A. Kulkarni

Beilstein J. Org. Chem. 2014, 10, 405–424, doi:10.3762/bjoc.10.38

• , pharmaceuticals, fuel additives, antioxidants, and rubber accelerators. In the leather industry m-nitrophenol is used as a fungicide and p-nitrophenol as a chemical intermediate for leather preservatives. 2,4-Dinitrophenol is useful for the manufacturing of photographic developers and serves as a wood

The myxocoumarins A and B from Stigmatella aurantiaca strain MYX-030

• Tobias A. M. Gulder,
• Snežana Neff,
• Traugott Schüz,
• Tammo Winkler,
• René Gees and
• Bettina Böhlendorf

Beilstein J. Org. Chem. 2013, 9, 2579–2585, doi:10.3762/bjoc.9.293

• with cell membrane stability [21]. Inhibition of acetyl-CoA carboxylase is exerted by soraphen A1α (2), which has been shown to be a potent and broad spectrum fungicide [22][23]. The most dominant target of myxobacterial antifungal agents, however, is the mitochondrial respiratory chain [21]. The

Theoretical study on β-cyclodextrin inclusion complexes with propiconazole and protonated propiconazole

• Adrian Fifere,
• Narcisa Marangoci,
• Stelian Maier,
• Adina Coroaba,
• Dan Maftei and
• Mariana Pinteala

Beilstein J. Org. Chem. 2012, 8, 2191–2201, doi:10.3762/bjoc.8.247

• methods consists of the complexation of antifungals with cyclodextrins and/or with soluble polymers. Propiconazole (PP) is a triazole derivative effective as a fungicide, with a broad spectrum, designed and launched by Janssen Pharmaceutics (Belgium). It is widely used in agriculture as a systemic foliar

• fungicide and, lately, for its fungistatic action. Propiconazole nitrate was tested in order to reduce the toxicity of the unmodified PP, but little information is available on this topic. Recently synthesized positively charged protonated propiconazole (PPH+) showed an increased antifungal activity