- Preparation method of isoxazole derivative
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The invention relates to a preparation method of an isoxazole derivative, which comprises the following steps of mixing an propargyl alcohol derivative, a halogen source, an acid and a solvent, and heating to react; adding the hydroxylamine into the react
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Paragraph 0060-0065
(2019/12/02)
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- Reactions of trans-1-(β-aroylvinyl)pyridinium bromides with hydroxylamine hydrochloride
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Reactions of trans-1-(β-aroylvinyl)pyridinium bromides with hydroxylamine hydrochloride lead to a mixture of substituted isoxazoles regardless of the substituent nature in the aromatic core and the solvent.
- Khachikyan, R. Dzh.,Hovakimyan,Panosyan,Tamazyan,Ayvazyan
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p. 1078 - 1081
(2015/06/25)
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- Efficient and regioselective one-pot synthesis of 3-substituted and 3,5-disubstituted isoxazoles
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(Figure Presented) A series of 3-substituted and 3,5-disubstituted isoxazoles have been efficiently synthesized in moderate to excellent yields by the reaction of N-hydroxyl-4-toluenesulfonamide with α,β-unsaturated aldehydes/ketones. This novel strategy is associated with readily available starting materials, mild conditions, high regioselectivity, and wide scope.
- Tang, Shibing,He, Jinmei,Sun, Yongquan,He, Liuer,She, Xuegong
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supporting information; experimental part
p. 3982 - 3985
(2009/12/03)
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- Synthesis of azirines containing aldehyde functionality and their utilization as synthetic tools for five membered oxazoles and isoxazoles
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(Chemical Equation Presented) A simple and useful procedure for the synthesis of azirines containing aldehyde functionality from open chain bromo/chloro-aldehydes at room temperature is reported. The scope of the ring expansion reaction of a number of 3-s
- Brahma, Sulagna,Ray, Jayanta K.
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p. 311 - 317
(2008/09/20)
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- Reaction of β-dimethylaminovinyl ketones with hydroxylamine: A simple and useful method for synthesis of 3- and 5-substituted isoxazoles
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(Chemical Equation Presented) The regioselective synthesis of 3- and 5-substituted-isoxazoles from the reaction of β-dimethylaminovinyl ketones [R-C(O)CH=CH-NMe2, where R = Ph, MeO-4-C6H4, F-4-C6H4, C
- Rosa, Fernanda A.,Machado, Pablo,Bonacorso, Helio G.,Zanatta, Nilo,Martins, Marcos A. P.
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p. 879 - 885
(2008/09/21)
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- Substituent effects on 15N and 13C NMR chemical shifts of 3-phenylisoxazoles: A theoretical and spectroscopic study
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The synthesis and assignment of 15N and 13C NMR signals of the isoxazole ring in a series of parasubstituted 3-phenyl derivatives are reported. DFT calculations of 15N and 13C chemical shifts are presented and c
- Schofield, Mark H.,Sorel, Marie-Adele,Manalansan, Ryan J.,Richardson, David P.,Markgraf, J. Hodge
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p. 851 - 855
(2007/10/03)
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- Amides that inhibit vanilloid receptor subtype 1 (VR1) receptor
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The present invention relates to compounds of formula (I) that are novel VR1 antagonists useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.
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- A convenient and expedient synthesis of 3-aryl-2H-azirine-2-carboxaldehydes
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A new procedure for the synthesis of 3-aryl-2H-azirine-2-carboxaldehydes starting from cinnamyl alcohols is disclosed. This novel approach implies milder conditions and higher overall yields as compared to the previously reported methods. The key step, i.e. the formation of the azirine ring, involves the treatment of (Z)-3-aryl-3-azidoprop-2-en-1-ols with MnO2.
- Alajari?n, Mateo,Orenes, Rau?l-A?ngel,Vidal, A?ngel,Pastor, Aurelia
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- SUBSTITUTED BIPHENYL ISOXAZOLE SULFONAMIDES
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Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R 1, R 2, R 3 and R 4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy,
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- Substituted biphenyl isoxazole sulfonamides
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Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R1, R2, R3 and R4 are each directly bonded to a ring carbon and are each independently (a) hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3 ; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) --C(O)H or --C(O)R5 ; (h) --CO2 H or --CO2 R5 ; (i) --Z4 --NR6 R7 ; (j) --Z4 --N(R10)--Z5 --NR8 R9 ; or (k) R3 and R4 together may also be alkylene or alkenylene, either of which may be substituted with Z1, Z2 and Z3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; and the remaining symbols are as defined in the specification.
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- SUBSTITUTED BIPHENYL ISOXAZOLE SULFONAMIDES
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Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R 1, R 2, R 3 and R 4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy,
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- SYNTHESIS AND PROPERTIES OF AZOLS AND THEIR DERIVATIVES. PART VI. CYCLOADDITION REACTIONS OF NITROETHYLENE WITH AROMATIC NITRILE N-OXIDES AND SOME CONVERSIONS OF 3-ARYL-5-NITRO-4,5-DIHYDRO-1,2-OXAZOLES
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Reactions of aromatic nitrile N-oxides with nitroethylene lead to formation of 3-aryl-5-nitro-4,5-dihydro-1,2-oxazoles.During heating the above compounds decompose with elimination of nitrous acid, thus affording 3-aryl-1,2-oxazoles.Under nucleophilic reagents a ring opening was observed.
- Baranski, Andrzej,Shvekhgeimer, Genrikh A.
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p. 459 - 467
(2007/10/02)
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- 5-Amino-4,5-dihydroisoxazoles. Part I. 5-Amino-3-aryl-4-methylene-4,5-dihydroisoxazoles and 4-Aminomethyl-3-arylisoxazoles from 5-Amino-4-aminomethyl-3-aryl-4,5-dihydroisoxazoles
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5-Amino-4-aminomethyl-3-aryl-4,5-dihydroisoxazoles 2 were obtained by cycloaddition of nitrile oxides to 1,3-diaminopropenes 1.On reaction with methyliodide the corresponding 4-(quaternary)-ammoniomethyl iodides 3 were formed.These compounds, on reaction
- Pocar, Donato,Rossi, Luisa Maria,Trimarco, Pasqualina,Vago, Luciano
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p. 881 - 885
(2007/10/02)
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