2039-49-8Relevant articles and documents
Copper-Mediated Domino Cyclization/Trifluoromethylation of Propargylic N-Hydroxylamines: Synthesis of 4-Trifluoromethyl-4-isoxazolines
Wang, Quande,Tsui, Gavin Chit
, p. 2971 - 2979 (2018)
A Cu(OTf)2-mediated synthesis of trifluoromethylated 4-isoxazolines is described. In one step from readily available propargylic N-hydroxylamines, a domino 5-endo-dig cyclization, followed by trifluoromethylation, takes place to construct the 4-isoxazoline core with concomitant installation of the CF3 group at the C-4 position. Such compounds could also be useful precursors for the preparation of α-trifluoromethyl β-amino ketones.
One-pot synthesis of 5-phenylsulfonyl-3-aroylisoxazolines and 3-aroylisoxazoles from alkynes and (phenylsulfonyl)ethene
Wang, Liang,Zhang, Nana
, p. 390 - 392 (2021)
Iron(III) nitrate-assisted cycloaddition of (phenylsulfonyl)ethene to arylacetylenes in the presence of KI affords 5-phenylsulfonyl-3-aroylisoxazolines whose treatment with K2CO3 provides 4,5-unsubstituted 3-aroylisoxazoles. Both synthetic steps can be performed in a one-pot manner.
Aerobic oxidative synthesis of 3,5-disubstituted isoxazoles directly from α,β-unsaturated ketones
Li, Zheng,Wen, Gong,Fu, Rugang,Yang, Jingya
, p. 643 - 644 (2016)
Using an efficient aerobic oxidative method, the synthesis of ten 3,5-disubstituted isoxazoles by treatment of α,β-unsaturated ketones with hydroxylamine and NaOH at room temperature has been achieved.
5-Substituted pyridylisoxazoles as effective inhibitors of platelet aggregation
Demina,Khodonov,Sinauridze,Shvets,Varfolomeev
, p. 2092 - 2113 (2014)
A series of 5-substituted 3-pyridylisoxazoles were synthesized using [3+2] cycloaddition of nitrile oxides to alkynes with variation of substituents at position 5 of the isoxazole ring without additional synthetic stages and with retention of 2-pyridyl-, 3-pyridyl, and 4-pyridyl substituents at position 3 of the isoxazole ring. Substituted pyridylisoxazoles are the potential antiaggregatory agents showing in vitro activity in the concentration range from 1?10-6 mol L-1 to 1?10-4 mol L-1 toward the human platelet rich blood plasma with arachidonic acid being used as the inductor of aggregation. These compounds do not act as cyclooxygenase or thromboxane synthase inhibitors, nor as thrombin inhibitors.
3, 5-disubstituted isoxazole derivative and synthesis method thereof
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Paragraph 0011; 0023-0024, (2021/08/14)
The invention provides a 3, 5-disubstituted isoxazole derivative and a synthesis method thereof, and belongs to the technical field of organic synthesis medicines and medical intermediates. The method comprises the following steps: adding a proper solvent
TEMPO-Mediated Selective Synthesis of Isoxazolines, 5-Hydroxy-2-isoxazolines, and Isoxazoles via Aliphatic δ-C(sp3)-H Bond Oxidation of Oximes
Mondal, Santanu,Biswas, Sourabh,Ghosh, Krishna Gopal,Sureshkumar, Devarajulu
, p. 2439 - 2446 (2021/08/03)
Selective synthesis of three different bioactive heterocycles; isoxazolines, 5-hydroxy-2-isoxazolines and isoxazoles from the same starting material using TEMPO (2,2,6,6-Tetramethylpiperidin-1-oxyl) as a radical initiator is reported. Selectivity was achi