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Journal articles on the topic 'Isoxazoles'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

Fuse, Shinichiro, Taiki Morita, and Hiroyuki Nakamura. "Step-by-Step Multifunctionalization of Isoxazoles Based On SEAr Reactions and C–H Direct Arylations." Synthesis 49, no. 11 (2017): 2351–60. http://dx.doi.org/10.1055/s-0036-1588784.

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Functionalized isoxazoles are important as pharmaceuticals and agrochemicals. Generally, electrophilic aromatic substitution or generation of carbanions/electrophilic trapping approach is used to introduce functional groups into unsubstituted heteroaromatics. However, these approaches have not been simple to apply to unsubstituted isoxazoles due to their poor nucleophilicity and instability under basic conditions. Recently several approaches have been reported to overcome these problems. This review summarizes the functionalization of isoxazoles, including SEAr reactions and C–H direct arylati

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2

Wang, Xiyue, Qingyun Hu, Hui Tang, and Xinhui Pan. "Isoxazole/Isoxazoline Skeleton in the Structural Modification of Natural Products: A Review." Pharmaceuticals 16, no. 2 (2023): 228. http://dx.doi.org/10.3390/ph16020228.

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Isoxazoles and isoxazolines are five-membered heterocyclic molecules containing nitrogen and oxygen. Isoxazole and isoxazoline are the most popular heterocyclic compounds for developing novel drug candidates. Over 80 molecules with a broad range of bioactivities, including antitumor, antibacterial, anti-inflammatory, antidiabetic, cardiovascular, and other activities, were reviewed. A review of recent studies on the use of isoxazoles and isoxazolines moiety derivative activities for natural products is presented here, focusing on the parameters that affect the bioactivity of these compounds.

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3

Yoshimura, Akira, Akio Saito, Viktor V. Zhdankin, and Mekhman S. Yusubov. "Synthesis of Oxazoline and Oxazole Derivatives by Hypervalent-Iodine-Mediated Oxidative Cycloaddition Reactions." Synthesis 52, no. 16 (2020): 2299–310. http://dx.doi.org/10.1055/s-0040-1707122.

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Organohypervalent iodine reagents are widely used for the preparation of various oxazolines, oxazoles, isoxazolines, and isoxazoles. In the formation of these heterocyclic compounds, hypervalent iodine species can serve as the activating reagents for various substrates, as well as the heteroatom donor reagents. In recent research, both chemical and electrochemical approaches toward generation of hypervalent iodine species have been utilized. The in situ generated active species can react with appropriate substrates to give the corresponding heterocyclic products. In this short review, we summa

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4

Fershtat, Leonid L., Daniil A. Chaplygin, Ivan V. Ananyev, and Nina N. Makhova. "Divergent Synthesis of Five-Membered Nitrogen Heterocycles via Cascade Reactions of 4-Arylfuroxans." Synthesis 52, no. 18 (2020): 2667–78. http://dx.doi.org/10.1055/s-0040-1707393.

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A novel method for the synthesis of a diverse series of functionally substituted five-membered heterocyclic compounds via atom-economic, regio-, and diastereoselective one-pot reaction cascade was developed. This approach involves a ring opening in 4-arylfuroxans to α-oximinoarylacetonitrile oxides followed by [3+2] cycloaddition to various dipolarophiles to afford multisubstituted isoxazoles and isoxazolines. Subsequent azole–azole rearrangement of (oximino)isoxazolines/-isoxazoles, which can be conducted in a one-pot manner, results into functionally substituted furazans formation. The devel

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5

Chikkula, Krishna Veni, and Raja S. "ISOXAZOLE – A POTENT PHARMACOPHORE." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 7 (2017): 13. http://dx.doi.org/10.22159/ijpps.2017.v9i7.19097.

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Isoxazole is an azole with an oxygen atom next to the nitrogen. Isoxazole rings are found in some natural products, such as ibotenic acid and also found in a number of drugs, including COX-2 inhibitor valdecoxib. Furoxan, a nitric oxide donor is containing isoxazolyl group & found in many β-lactamase resistant antibiotics, such as cloxacillin, dicloxacillin and flucloxacillin. The synthetic androgenic steroid danazol also has an isoxazole ring. The substituted isoxazoles are well developed in literature to posses significant biological activities. The disubstituted and trisubstituted isoxa

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6

Zawadzińska-Wrochniak, Karolina, Isabelle Zavecz, and Serhii Hirka. "The recent progress in the field of the applications of isoxazoles and their hydrogenated analogs: mini review." Scientiae Radices 3, no. 4 (2024): 228–47. https://doi.org/10.58332/scirad2024v3i4a01.

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Recent review of the general application of isoxazoles and isoxazolines has been done based on current state of the art in this area. Isoxazole and its analogues have majority of possible applications in many fields of plural branches of industry. They possess good biological activity, so most of them are being used successfully in medicine and veterinary. These heterocyclic compounds could be also very important precursors of many organic transformation. Due to their easy modification, general interest of their development still increases.

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7

Cao, Jian-Kang, Tian-Zheng Cao, Qian-Wen Yue, et al. "tert-Butyl Nitrite-Induced Radical Nitrile Oxidation Cycloaddition: Synthesis of Isoxazole/Isoxazoline-Fused Benzo 6/7/8-membered Oxacyclic Ketones." Molecules 29, no. 6 (2024): 1202. http://dx.doi.org/10.3390/molecules29061202.

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A practical metal-free and additive-free approach for the synthesis of 6/7/8-membered oxacyclic ketone-fused isoxazoles/isoxazolines tetracyclic or tricyclic structures is reported through Csp3–H bond radical nitrile oxidation and the intramolecular cycloaddition of alkenyl/alkynyl-substituted aryl methyl ketones. This convenient approach enables the simultaneous formation of isoxazole/isoxazoline and 6/7/8-membered oxacyclic ketones to form polycyclic architectures by using tert-butyl nitrite (TBN) as a non-metallic radical initiator and N–O fragment donor.

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8

Griesbeck, Axel G., Marco Franke, Jörg Neudörfl, and Hidehiro Kotaka. "Photocycloaddition of aromatic and aliphatic aldehydes to isoxazoles: Cycloaddition reactivity and stability studies." Beilstein Journal of Organic Chemistry 7 (January 26, 2011): 127–34. http://dx.doi.org/10.3762/bjoc.7.18.

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The first photocycloadditions of aromatic and aliphatic aldehydes to methylated isoxazoles are reported. The reactions lead solely to the exo-adducts with high regio- and diastereoselectivities. Ring methylation of the isoxazole substrates is crucial for high conversions and product stability. The 6-arylated bicyclic oxetanes 9a–9c were characterized by X-ray structure analyses and showed the highest thermal stabilities. All oxetanes formed from isoxazoles were highly acid-sensitive and also thermally unstable. Cleavage to the original substrates is dominant and the isoxazole derived oxetanes

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9

M. Ahmed, Sarbast, Hewa Omer Ahmed, Faiq H. S. Hussain, Hayman Sardar Abdulrahman, and Hemn A. Qader. "Synthesis and Antimicrobial Activity of some Ester Functionalized Isoxazoles incorporating Anthracene Moieties via Nucleophilic Substitution Reaction." Zanco Journal of Medical Sciences 27, no. 2 (2023): 213–26. http://dx.doi.org/10.15218/zjms.2023.024.

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Background and objective: Five-membered heterocycle compounds having single oxygen and nitrogen atom at adjacent positions are known as isoxazoles. Isoxazole compounds have a broad range of biological activities and therapeutic value. In view of a strategic design of antimicrobial compounds, several new ester-functionalized isoxazoles were synthesized and characterized. Methods: A regioselective isoxazole incorporating an anthracene moiety was adducted via an effective 1,3-dipolar cycloaddition between anthracene nitrile oxide and propargyl bromide as a dipolarophile. Results: Synthesized isox

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10

Thirunarayanan, G., and V. Sathiyendiran. "Synthesis, Pharmacological and Insect Antifeedant Activities of some 3-(2-Naphthyl)-5-(Substituted Phenyl)-4,5-Dihydroisoxazoles." International Letters of Chemistry, Physics and Astronomy 49 (April 2015): 1–14. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.49.1.

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Totally thirty one 3,5-substituted aryl 4,5-dihydro isoxazole derivatives including 3-(2-naphthyl)-5-(substituted phenyl)-4,5-dihydroisoxazole have been synthesized by fly-ash:H2SO4 catalyzed cyclization of hydroxylamine hydrochloride and aryl chalcones under solvent-free conditions. The yields of the isoxazoles are more than 94%. The synthesized isoxazole were characterized by their physical constants and spectral data. The antimicrobial, antioxidant and insect antifeedant activities of the synthesized isoxazoles have been evaluated using a variety of bacterial and fungal species, DPPH radica

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11

Thirunarayanan, G., and V. Sathiyendiran. "Synthesis, Pharmacological and Insect Antifeedant Activities of some 3-(2-Naphthyl)-5-(Substituted Phenyl)-4,5-Dihydroisoxazoles." International Letters of Chemistry, Physics and Astronomy 49 (April 7, 2015): 1–14. http://dx.doi.org/10.56431/p-g0r04d.

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Totally thirty one 3,5-substituted aryl 4,5-dihydro isoxazole derivatives including 3-(2-naphthyl)-5-(substituted phenyl)-4,5-dihydroisoxazole have been synthesized by fly-ash:H2SO4 catalyzed cyclization of hydroxylamine hydrochloride and aryl chalcones under solvent-free conditions. The yields of the isoxazoles are more than 94%. The synthesized isoxazole were characterized by their physical constants and spectral data. The antimicrobial, antioxidant and insect antifeedant activities of the synthesized isoxazoles have been evaluated using a variety of bacterial and fungal species, DPPH radica

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12

Cherton, Jean-Claude, Marc Lanson, Daïf Ladjama, Yvette Guichon та Jean-Jacques Basselier. "Synthèse d'isoxazoles substitués en α de l'azote par une chaine alkyle ou alcényle". Canadian Journal of Chemistry 68, № 8 (1990): 1271–76. http://dx.doi.org/10.1139/v90-196.

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Several syntheses of special isoxazoles bearing a long alkyl or alkenyl side chain in the α position of the nitrogen are presented. A very convenient route in the case of an alkyl side chain is the classical 1,3-dipolar cycloaddition of a nitrile-oxide to a vinyl acetate. Although it is a rather long approach, the reaction of hydroxylamine with enone-epoxides represents a new and unequivocal method compatible with alkenyl side chains. The isomerisation of the easily synthesized isoxazoles bearing such substitutents α to the oxygen, by the reaction of their isoxazolium salts with hydroxylamine,

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13

Kumar, Pravin. "Regioselektywna C-H funkcjonalizacja izoksazoli katalizowana metalami przejściowymi: postęp i spostrzeżenia mechanistyczne." Wiadomości Chemiczne 79, no. 5-6 (2025): 359–79. https://doi.org/10.53584/wiadchem.2025.05.4.

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Isoxazoles are a versatile heteroaromatic scaffold prevalent in various life-saving drugs, pharmaceuticals, and biologically active natural products. Transition metal-catalyzed C−H functionalization of isoxazole has gained significant attention due to its potential for direct modification without pre-functionalization. This review highlights the recent advances in the regioselective C−H functionalization of isoxazoles, focusing on the catalyst system, directing group strategy, and mechanistic understanding.

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14

Ouzounthanasis, Konstantinos A., Jasmina Glamočlija, Ana Ćirić, and Alexandros E. Koumbis. "Studies of the Synthesis of Fused Isoxazoline/Isoquinolinones and Evaluation of the Antifungal Activity of Isoxazole-like Benzamide and Isoquinolinone Hybrids." Molecules 30, no. 3 (2025): 589. https://doi.org/10.3390/molecules30030589.

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Isoxazole derivatives (isoxazoles, isoxazolines, and isoxazolidines) are present in the structure of several natural products and/or pharmaceutically interesting compounds. In this work, a synthetic study for the preparation of fused isoxazoline/isoquinolinone hybrids is presented. The initial approach involving the sequential 1,3-dipolar cycloaddition of nitrile oxides to indenone (to obtain the isoxazoline ring) and a Beckmann rearrangement (to construct the isoquinolinone lactam system) was complicated by the formation of fragmentation products during the latter. Therefore, the desired hybr

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15

Svejstrup, Thomas D., Wojciech Zawodny, James J. Douglas, Damon Bidgeli, Nadeem S. Sheikh, and Daniele Leonori. "Visible-light-mediated generation of nitrile oxides for the photoredox synthesis of isoxazolines and isoxazoles." Chemical Communications 52, no. 83 (2016): 12302–5. http://dx.doi.org/10.1039/c6cc06029c.

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16

Camoutsis, Ch, and S. Nikolaropoulos. "Steroidal isoxazoles, isoxazolines and isoxazolidines." Journal of Heterocyclic Chemistry 35, no. 4 (1998): 731–59. http://dx.doi.org/10.1002/jhet.5570350401.

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17

Dudik, Alexander S., Timur O. Zanakhov, Ekaterina E. Galenko, Mikhail S. Novikov, and Alexander F. Khlebnikov. "Azirinyl-Substituted Nitrile Oxides: Generation and Use in the Synthesis of Isoxazole Containing Heterocyclic Hybrids." Molecules 30, no. 13 (2025): 2834. https://doi.org/10.3390/molecules30132834.

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The procedure for the generation of azirinyl-substituted nitrile oxides by the reaction of 2-(diazoacetyl)-2H-azirines with tert-butyl nitrite while preserving the azirine ring has been developed. The [3+2] cycloaddition of azirinyl-substituted nitrile oxides to terminal acetylenes produced azirinyl(isoxazolyl)ketones with various substituents in position 3 of azirine and position 5 of isoxazole fragments in a 51–91% yield at room temperature in DCM. DFT calculations and experimental data are consistent with the assumption that the formation of azirinyl-substituted nitrile oxides is accelerate

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18

Rey, Marine, and Stéphane Beaumont. "Molybdenum-Mediated One-Pot Synthesis of Pyrazoles from Isoxazoles." Synthesis 51, no. 20 (2019): 3796–804. http://dx.doi.org/10.1055/s-0039-1690615.

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A one-pot approach for the direct synthesis of substituted pyrazoles from isoxazoles is reported. The process involves isoxazole N–O bond cleavage mediated by a molybdenum complex, in situ hydrolysis of the resulting β-amino enone to the corresponding 1,3-diketone, followed by pyrazole formation in the presence of hydrazine or substituted hydrazine. Good to excellent yields and regioselectivities are obtained with nonsymmetric isoxazoles. By using readily available starting materials, a wide range of substituted pyrazoles may be synthesized by this method.

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19

Pajkert, Romana, Henryk Koroniak, Paweł Kafarski, and Gerd-Volker Röschenthaler. "Hypervalent-iodine mediated one-pot synthesis of isoxazolines and isoxazoles bearing a difluoromethyl phosphonate moiety." Organic & Biomolecular Chemistry 19, no. 22 (2021): 4871–76. http://dx.doi.org/10.1039/d1ob00685a.

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20

Lin, Yifan, Ke Zhang, Mingchun Gao, et al. "Copper nitrate-mediated synthesis of 3-aryl isoxazolines and isoxazoles from olefinic azlactones." Organic & Biomolecular Chemistry 17, no. 22 (2019): 5509–13. http://dx.doi.org/10.1039/c9ob00857h.

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21

Das, Soumyadip, and Kaushik Chanda. "An overview of metal-free synthetic routes to isoxazoles: the privileged scaffold." RSC Advances 11, no. 52 (2021): 32680–705. http://dx.doi.org/10.1039/d1ra04624a.

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Isoxazole, a five-membered heterocyclic moiety commonly found in many commercially available drugs. This review article presents a comprehensive overview on metal-free synthetic routes for the synthesis of isoxazoles with significant bioactivities.

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22

Kumar, Pravin, and Manmohan Kapur. "Ruthenium-catalyzed oxidative coupling of vinylene carbonate with isoxazoles: access to fused anthranils." Chemical Communications 58, no. 28 (2022): 4476–79. http://dx.doi.org/10.1039/d2cc01048h.

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A ruthenium-catalyzed oxidative coupling of vinylene carbonate with isoxazoles has been developed to achieve the direct C–H formylmethylation of a diverse array of arylisoxazoles utilizing the isoxazole ring as the directing group.

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23

Ravindra, M. V., S. Suvarna, and C. S. Ananda Kumar. "Synthesis of Unusually Substituted 2,4,5-Trimethoxy 3,5-Diaryl Isoxazoles from Natural Precursor: Antimicrobial and Anticancer Activities." Asian Journal of Chemistry 36, no. 2 (2024): 458–64. http://dx.doi.org/10.14233/ajchem.2024.31015.

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In this work, 2,4,5-trimethoxy substituted 3,5-diaryl isoxazoles were synthesized via their chalcone intermediates and evaluated for antimicrobial and anticancer activities. The natural precursor 2,4,5-trimethoxy benzaldehyde (asaronaldehyde) was obtained from oxidation of β-asarone (Acorus calamus oil) and then reacted with substituted acetophenones via Claisen-Schmidt condensation yielded 2,4,5-trimethoxy substituted chalcones. These chalcones on further treatment with hydroxylamine in presence of sodium acetate and acetic acid cyclizes to give the corresponding 3,5-diaryl isoxazoles yields

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24

Mohammed, Shabber, Ram A. Vishwakarma, and Sandip B. Bharate. "Metal-free DBU promoted regioselective synthesis of isoxazoles and isoxazolines." RSC Advances 5, no. 5 (2015): 3470–73. http://dx.doi.org/10.1039/c4ra14694h.

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25

Liu, Hui, Yingkun Yan, Jiayan Zhang, et al. "Enantioselective dearomative [3+2] annulation of 5-amino-isoxazoles with quinone monoimines." Chemical Communications 56, no. 88 (2020): 13591–94. http://dx.doi.org/10.1039/d0cc05807f.

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Enantioselective dearomative [3+2] annulation of 5-amino-isoxazoles with quinone monoimines provided various (bridged) isoxazolines fused dihydrobenzofurans with moderate to good yields in moderate to good enantioselectivities.

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26

Pramanik, Nabyendu, Satinath Sarkar, Dipanwita Roy, et al. "Synthesis and diverse general oxidative cyclization catalysis of high-valent MoVIO2(HL) to ubiquitous heterocycles and their chiral analogues with high selectivity." RSC Advances 5, no. 123 (2015): 101959–64. http://dx.doi.org/10.1039/c5ra21825j.

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The first synthesis and diverse oxidative cyclization catalysis properties of high-valent Mo<sup>VI</sup>–triazole are demonstrated towards highly selective construction of benzimidazoles, benzothiazoles, isoxazolines, isoxazoles and their chiral analogues.

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27

Obydennov, Dmitrii L., Asmaa I. El-Tantawy, and Vyacheslav Ya Sosnovskikh. "Bio-based triacetic acid lactone in the synthesis of azaheterocyclesviaa ring-opening transformation." New Journal of Chemistry 42, no. 11 (2018): 8943–52. http://dx.doi.org/10.1039/c8nj01044g.

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In the present article a new way of converting biobased triacetic acid lactone (TAL) into azaheterocyclic compounds, such as 4-pyridones, pyrazoles, isoxazolines and isoxazoles, has been found through reactive and multifunctional polycarbonyl intermediates.

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28

Karthikeyan, K., R. Senthil Kumar, P. Dheenkumar, and Paramasivan T. Perumal. "Solvent and catalyst free route to 3-indolyl glycoconjugates: synthesis of sugar tethered isoxazolines and isoxazoles from 3-indolyl nitroalkanes." RSC Adv. 4, no. 53 (2014): 27988–97. http://dx.doi.org/10.1039/c4ra02825b.

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An expedient, solvent and catalyst free strategy for the synthesis of sugar based bis(indolyl)methanes and indolyl nitroalkanes has been developed. Further, the nitroalkanes were converted to novel isoxazolines and isoxazoles by nitrile oxides cycloaddition.

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29

Al-Zaydi, Khadijah Mohamed, and Ebtisam Abdel Aziz Hafez. "1,3-Dipolar Cycloadditions of Some Nitrilimines and Nitrile Oxides to 3-N,N-Dimethylamino-1 -oxopropene Derivatives." Journal of Chemical Research 23, no. 6 (1999): 360–61. http://dx.doi.org/10.1177/174751989902300608.

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An efficient synthesis of some novel pyrazoles 8a-j, 13a-e, 18a,b, isoxazoles 26a-g, pyrazolo[3,4- d]pyridazines 9a-d and isoxazolo[3,4- d]pyridazines 27a-d via 1,3-dipolar cycloaddition reactions is reported.

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30

Beccalli, E. M., A. Marchesini, and T. Pilati. "Oxazolo[4,5-d]isoxazole Derivatives and 3,4-Disubstituted Isoxazoles from Isoxazol-5(4H)-ones." Synthetic Communications 23, no. 5 (1993): 685–702. http://dx.doi.org/10.1080/00397919308009828.

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31

De Micheli, Carlo, Patrizia Caldirola, Marco De Amichi, and Paolo Pevarello. "An Efficient Synthesis of Isoxazoles and Isoxazolines." HETEROCYCLES 23, no. 10 (1985): 2479. http://dx.doi.org/10.3987/r-1985-10-2479.

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32

Pruitt, James R., Donald J. Pinto, Melissa J. Estrella, et al. "Isoxazolines and isoxazoles as factor Xa inhibitors." Bioorganic & Medicinal Chemistry Letters 10, no. 8 (2000): 685–89. http://dx.doi.org/10.1016/s0960-894x(00)00097-4.

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33

CAMOUTSIS, CH, and S. NIKOLAROPOULOS. "ChemInform Abstract: Steroidal Isoxazoles, Isoxazolines and Isoxazolidines." ChemInform 29, no. 52 (2010): no. http://dx.doi.org/10.1002/chin.199852329.

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34

Kumar, Vinod, and Kamalneet Kaur. "Fluorinated isoxazolines and isoxazoles: A synthetic perspective." Journal of Fluorine Chemistry 180 (December 2015): 55–97. http://dx.doi.org/10.1016/j.jfluchem.2015.09.004.

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35

Sharma, Aruna, Anjali Yadav, Hardik Pathak, Bhawana Jangir, and Rahul Goel. "Effective synthesis and pharmacological evaluation of 1,2,4-triazolo-isoxazole and 1,2,4-triazolo-pyrazole scaffolds." Research Journal of Chemistry and Environment 29, no. 5 (2025): 77–82. https://doi.org/10.25303/295rjce077082.

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Five-membered heteroaromatic compounds like pyrazoles and isoxazoles are significant for the pharmaceutical sector and material research, becoming more significant in drug research, cosmetics as well as in the creation of agricultural products. 1,2,4-triazolo fused isoxazole derivatives (3a-f) were synthesized from reaction between intermediate chal cone-1,2,4-triazolo-1,5-benzodiazepine derivatives 2af with hydroxyl amine hydrochloride. 1,2,4-triazolo fused pyrazole derivatives (3a-f and 4a-f) were prepared from reaction between chalcone derivatives 2a-f with hydrazine hydrate and its phenyl

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36

Jedlovská, Eva, Lubor Fišera, Anna Balková, Jaroslav Kováč, and Ladislav Štibrányi. "Cycloadditions of 2,5-dimethyl-3-furannitrile oxide to alkenes and alkynes." Collection of Czechoslovak Chemical Communications 55, no. 10 (1990): 2481–92. http://dx.doi.org/10.1135/cccc19902481.

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Regioselectivity of 1,3-dipolar cycloadditions of 2,5-dimethyl-3-furannitrile oxide (IIa) to alkenes or alkynes is described. Nitrile oxide IIa generated in situ reacts with monosubstituted alkenes or alkynes to give exclusively 5-substituted 3-(5-dimethyl-3 -furyl)-2-isoxazolines IV and isoxazoles V, 2,5-disubstituted alkenes sometimes afforded a mixture of regioisomeric isoxazolines. Reactivity of furannitrile oxides II and III in cycloadditions to ethene was studied by the MNDO method.

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37

Vasilenko, Dmitry A., Nadezhda S. Temnyakova, Sevastian E. Dronov, et al. "5-Nitroisoxazoles in SNAr Reactions: A Novel Chemo- and Regioselective Approach to Isoxazole-Based Bivalent Ligands of AMPA Receptors." International Journal of Molecular Sciences 24, no. 22 (2023): 16135. http://dx.doi.org/10.3390/ijms242216135.

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An efficient regioselective approach to novel functionalized bis(isoxazoles) with a variety of aromatic and aliphatic linkers was elaborated, based on the heterocyclization reaction of electrophilic alkenes under the treatment with tetranitromethane-triethylamine complex affording 3-EWG-5-nitroisoxazoles. The subsequent SNAr reactions of 5-nitroisoxazoles with various O,O-, N,N- and S,S-bis(nucleophiles) provide a wide range of bis(isoxazole) derivatives in good isolated yields. Employing an elaborated method, a series of novel bis(3-EWG-isoxazoles) as the promising allosteric modulators of AM

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38

Chernikova, I. B., M. S. Yunusov, and A. N. Lobov. "Synthesis of 2-isoxazolines and isoxazoles with uracil fragments." Журнал органической химии 59, no. 6 (2023): 824–28. http://dx.doi.org/10.31857/s0514749223060137.

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By 1,3-dipolar cycloaddition to nitrile N -oxide obtained from 6-methyluracyl-5-carboxymidoyl chloride, compounds containing an allyl component or propargyl alcohol, a number of 2-isoxazolines and isoxazole with uracil fragments were synthesized.

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39

Duc, Dau Xuan, and Vo Cong Dung. "Recent Progress in the Synthesis of Isoxazoles." Current Organic Chemistry 25, no. 24 (2021): 2938–89. http://dx.doi.org/10.2174/1385272825666211118104213.

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Isoxazole derivatives are aromatic five-membered ring heterocyclic compounds with one oxygen atom and one nitrogen atom at adjacent positions. These compounds have a broad spectrum of applications in medicinal chemistry, such as antimicrobial, anticancer, antitumor, antitubercular, analgesic, anti-inflammatory, antidepressant, and anticonvulsant activities and some of them are well-known drugs for the treatment of various diseases in the market. The use of this class of compounds in agriculture as herbicides, insecticides have been widely reported. In organic materials, these compounds have be

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Ahmed, Sarbast, Hayman Abdulrahman, Faiq Hussain, Hiwa Ahmad, Idrees Qader, and Hemn Qader. "Synthesis, characterization and biological activity of some isoxazole derivatives via 1,3-dipolar cycloaddition reaction of nitrile oxide." Zanco Journal of Medical Sciences 29, no. 1 (2025): 137–53. https://doi.org/10.15218/zjms.2025.015.

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Background and objective: Isoxazoles are significant heterocyclic products that are used in various applications in the field of medicinal chemistry. Along with prescription drugs, a variety of bioactive pharmaceutical substances, such as valdecoxib, leflunomide, and danazol, include the isoxazole core. The present work aimed to synthesize and test the antibacterial, antioxidant, and antifungal activities combined with the theoretical investigations. Methods: Various 2,4-disubstituted isoxazoles have been synthesized through a 1,3-dipolar cycloaddition reaction via nitrile oxide. The structure

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Mahalanabis, Kumar K., S. K. Dutta Chowdhury, Mili Sarkar, and Manisha Misra. "Synthesis of substituted isoxazolones and isoxazoles from cyanoenaminones." Journal of Chemical Research 2006, no. 2 (2006): 78–80. http://dx.doi.org/10.3184/030823406776330864.

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Sammelson, Robert, Daniel Miller, and Christopher Bailey. "Synthesis of Isoxazolines and Isoxazoles Inspired by Fipronil." Synthesis 47, no. 18 (2015): 2791–98. http://dx.doi.org/10.1055/s-0034-1378737.

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Pan, Xinhui, Xiaobing Xin, Ying Mao та ін. "3-Benzoylisoxazolines by 1,3-Dipolar Cycloaddition: Chloramine-T-Catalyzed Condensation of α-Nitroketones with Dipolarophiles". Molecules 26, № 12 (2021): 3491. http://dx.doi.org/10.3390/molecules26123491.

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In this study, 3-benzoylisoxazolines were synthesized by reacting alkenes with various α-nitroketones using chloramine-T as the base. The scope of α-nitroketones and alkenes is extensive, including different alkenes and alkynes to form various isoxazolines and isoxazoles. The use of chloramine-T, as the low-cost, easily handled, moderate base for 1,3-dipolar cycloaddition is attractive.

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S. Abibindhu, Smitha Nair, and C. Kannan. "SYNTHESIS AND ANTI-INFLAMMATORY, ANTIOXIDANT STUDIES OF NOVEL CHALCONES-BASED ISOXAZOLE DERIVATIVES." RASAYAN Journal of Chemistry 15, no. 04 (2022): 2661–65. http://dx.doi.org/10.31788/rjc.2022.1547023.

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Our previous work identified various novel Chalcones (I-III) produced by mixing the equimolar amount of Ferrocene aldehyde and different substituted acetophenones which has a strong base. Hence, in the present study, novel various Chalcones (I-III) were treated with hydroxylamine hydrochloride to form various Isoxazoles (Ic-IIIc). The synthesized novel chalcone-based Isoxazole derivatives were determined by spectroscopic techniques such as1H,13C-NMR, FT-IR,and UV. Further, these products were evaluated for antimicrobial studies and antioxidant susceptibilities through DPPH radical scavenging m

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Saleem, Tahira, Muhammad Humble Khalid Tareen, Muhammad Rashid, et al. "REVIEW ON THE SYNTHESIS AND POTENTIAL THERAPEUTIC APPLICATIONS OF HETEROCYCLIC PRODUCTS OF 5-AMINO-3-METHYLISOXAZOLE." International Journal of Scientific & Engineering Research 12, no. 08 (2021): 154–72. http://dx.doi.org/10.14299/ijser.2021.08.01.

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In general, heterocyclic compounds have evoked interest and concern because of their fundamental role in biological profiles and biological actions in nature. Now, most of the lead molecules in medicinal chemistry are based on hetero-atoms. In medicinal chemistry- to bring two hetero-atoms to the drug molecule, isoxazoles are interesting functional groups. Isoxazole as a key building block has been widely used and is an important heterocyclic unit.

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BECCALLI, E. M., A. MARCHESINI, and T. PILATI. "ChemInform Abstract: Oxazolo(4,5-d)isoxazole Derivatives and 3,4-Disubstituted Isoxazoles from Isoxazol-5(4H)-ones." ChemInform 24, no. 26 (2010): no. http://dx.doi.org/10.1002/chin.199326129.

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V S, Anila Kumari, Dr Prasobh G R, and Sheeja Rekha A G. "A Brief Review on Isoxazole Derivatives as Antibacterial Agents." International Journal of Research and Review 9, no. 9 (2022): 321–33. http://dx.doi.org/10.52403/ijrr.20220935.

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Isoxazole compounds exhibit a wide spectrum of targets and broad biological activities. Isoxazole derivatives are still popular scaffolds for the development of new agents with variable biological activities such as antimicrobial, antiviral, anticancer, anti-inflammatory, immunomodulatory, anticonvulsant or antidiabetic properties. The key feature of these heterocycles is that they possess the typical properties of an aromatic system but contain a weak nitrogen-oxygen bond which under certain reaction conditions like reducing or basic conditions is a potential site of ring cleavage. Thus, isox

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V, Kumar, and Rao CMMP. "Pharmacological Screening of Some Novel 3,5-Disubstituted Isoxazoles Derivatives of Dibromochalcones." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 14, no. 04 (2024): 1130–38. https://doi.org/10.25258/ijddt.14.4.30.

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Background: The preparation of some novel 3, 5-disubstituted isoxazole derivatives of dibromochalcones is encouraged by the study. When hydroxylamine hydrochloride and α-β chalcone dibromide combine, a new technique for synthesizing 3,5-disubstituted isoxazoles is produced. Bromine or N-BromoSuccinimide can be used to produce compounds with low polarity like carbon tetrachloride, chloroform and dichloromethane; however the product obtained are very little. Tetrabutylammonium tribromide (TBABr3), thus, induces chalcones to bromate regioselectively and produces a high yield without polymerisatio

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Pruitt, James R., Donald J. Pinto, Melissa J. Estrella, et al. "ChemInform Abstract: Isoxazolines and Isoxazoles as Factor Xa Inhibitors." ChemInform 31, no. 30 (2010): no. http://dx.doi.org/10.1002/chin.200030111.

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Chukanov, N. V., S. A. Popov, G. V. Romanenko, and V. A. Reznikova. "Transformation of 1,2,3,7a-tetrahydroimidazo[1,2-b]isoxazole derivatives into isoxazoles." Russian Chemical Bulletin 56, no. 6 (2007): 1227–33. http://dx.doi.org/10.1007/s11172-007-0185-y.

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