91569-55-0Relevant academic research and scientific papers
Non-Decarboxylative Ruthenium-Catalyzed Rearrangement of 4-Alkylidene-isoxazol-5-ones to Pyrazole- and Isoxazole-4-carboxylic Acids
Loro, Camilla,Molteni, Letizia,Papis, Marta,Lo Presti, Leonardo,Foschi, Francesca,Beccalli, Egle M.,Broggini, Gianluigi
, p. 3092 - 3096 (2022/05/02)
Treatment of 4-(2-hydroaminoalkylidenyl)- and 4-(2-hydroxyalkylidenyl)-substituted isoxazol-5(4H)-ones with catalytic amounts of [RuCl2(p-cymene)]2, without any additive, afforded pyrazole- and isoxazole-4-carboxylic acids, respectively. The presence of an intramolecular H-bond in these substrates was the key to divert the classical mechanism toward a ring-opening non-decarboxylative path that is expected to generate a vinyl Ru-nitrenoid intermediate, the cyclization of which affords the rearranged products. A gram scale protocol demonstrated the synthetic applicability of this transformation.
Isoxazolo derivatives
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Page/Page column 14-15, (2008/06/13)
The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula wherein R1, R2, R3, R4, and R5, and m are as defined herein and with their phar
Aryl-isoxazol-4-yl-imidazole derivatives
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Page/Page column 16, (2010/11/28)
The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I: wherein R1 to R6 are as defmed in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds h
Aminoacetamide acyl guanidines as beta-secretase inhibitors
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Page/Page column 32, (2008/06/13)
There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R25, R26 and R27 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
Cardioactivity and solid-state structure of two 4-isoxazolyldihydropyridines related to the 4-aryldihydropyridine calcium-channel blockers
McKenna,Schlicksupp,Natale,Willett,Maryanoff,Flaim
, p. 473 - 476 (2007/10/02)
Diethyl 2,6-dimethyl-4-(5-ethyl-3-phenylisoxazol-4-yl)-1,4-dihydropyridine-3,5-dic arboxylate (5) and diethyl 2,6-dimethyl-4-(5-isopropyl-3-phenylisoxazol-4-yl)-1,4-dihydropyridine-3,5 -dicarboxylate (6) were synthesized, and their molecular structures we
Metalation of Isoxazolyloxazolines, a Facile Route to Functionally Complex Isoxazoles: Utility, Scope, and Comparison to Dianion Methodology
Natale, N. R.,McKenna, John I.,Niou, Chorng-Shyr,Borth, Mark,Hope, Hakon
, p. 5660 - 5666 (2007/10/02)
2-(5'-Alkylisoxazol-4'-yl)-Δ2-oxazoline was metalated at the C-5' alkyl group, and the lithio anion was quenched with a variety of electrophiles.Alkyl halides, aldehydes, and acylpyridinium salts were used as electrophiles.The lithio anion was oxygenated with MOOPH or N-(phenylsulfonyl)oxaziridene.The isoxazolyloxazoline system was converted to the isoxazolyl carboxylic acid, aldehyde, ketone, and chiral oxazoline.The isoxazolyloxazoline was formed, metalated, and deprotected in synthetically useful yields and represents a facile entry into functionally complex isoxazoles.To determine the necessity of the oxazoline protection/deprotection scheme, dianions of isoxazole-4-carboxylic acids were studied.The dianion method was found to be more efficient for simple alkyl halides, but limited in scope.
