- Green preparation method of isoxazole compound participating in water-soluble vitamin E
-
The invention provides a green synthesis method of an isoxazole compound represented by the formula (III), wherein the aldehyde oxime compound represented by the formula (I) is a substrate and is in an aqueous solution of a surfactant with a mass concentration 1 wt % - 5 wt % in N - chlorosuccinimide. The alkyne compound represented by the formula (II) is reacted 6 - 16h at room temperature under the common action of the basic substance, and the resulting reaction solution is post-treated to obtain the isoxazole compound represented by the formula (III). Water serves as a reaction solvent, the use amount of the organic solvent is reduced, and zero emission of the solvent is realized.
- -
-
Paragraph 0156-0159
(2021/11/03)
-
- On the reaction of sterically hindered α,β-unsaturated ketones with hydroxylamine: Preparation of 5-hydroxy derivatives of isoxazolidine and 4,5-dihydroisoxazole
-
A reaction of hydroxylamine with α,β-unsaturated ketones containing a tertiary carbon atom α to the keto group leads to 5-hydroxyisoxazolidine and 5-hydroxy-Δ2-isoxazoline derivatives.
- Mavrov,Firgang
-
p. 606 - 615
(2013/05/09)
-
- Synthesis and antiulcer activity of novel 5-(2-ethenyl substituted)-3(2H)- furanones
-
In order to investigate new antiulcer agents, spizofurone 1 (AG-629) was fragmented and reassembled to generate 5-phenyl-2,2-dimethyl-3(2H)-furanone (bullatenone, 2). Because of the antiulcer activity of 2,5-phenyl-substituted 2,2-dimethyl-3(2H)-furanones (3-6) were made and shown to have poor activity. Insertion of an ethenyl link between the furanone and phenyl rings gave 5-(2- phenylethenyl)-2,2-dimethyl-3(2H)-furanone (7). This compound had better activity than 2. Compounds 8-41 were synthesized to evaluate the SAR in 5-(2- ethenyl substituted)-3(2H)-furanones. Electron-withdrawing substituents on the aromatic ring (8, 10, 19, and 20) gave 2-3-fold higher activity. Further increases in the activity were found when the phenyl ring was replaced by heterocyclic nuclei. Compounds that contained a thiophene (29), pyridine (24- 26), or quinoline ring (32) had the best activity. Replacement of the methyl group on the furanone ring with a phenyl (34) or p-fluorophenyl (40) substituent in the 2-pyridine series gave compounds with activity that ranked with the best obtained in this study. The best compounds from the above SAR studies were evaluated in the ethanol-necrosis model for duration of cytoprotection action. Compounds 19, 24, and 29, which had the best duration of action, were tested with AG-629 in the acidified aspirin and indomethacin- induced lesion models. Only compound 24 had equivalent activity with AG-629 in both models.
- Felman,Jirkovsky,Memoli,Borella,Wells,Russell,Ward
-
p. 1183 - 1190
(2007/10/02)
-