- 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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- Harnessing Stereospecific Z-Enamides through Silver-Free Cp?Rh(III) Catalysis by Using Isoxazoles as Masked Electrophiles
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The stereospecific synthesis of Z-enamides is described in this paper. For the first time, isoxazoles have been employed as electrophiles in C-H functionalization to afford thermodynamically less stable Z-enamides utilizing salicylaldehydes in an atom- and step-economic fashion. The stereochemistry of enamides might originate from the relative disposition of atoms present in isoxazole and the intramolecular hydrogen bonding. The reaction showed excellent scope as several structurally and electronically diverse salicylaldehydes and isoxazoles reacted efficiently.
- Debbarma, Suvankar,Bera, Sourav Sekhar,Maji, Modhu Sudan
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p. 835 - 839
(2019/01/26)
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- A novel synthesis of 5-substituted isoxazoles from propargylic amines and N-hydroxyphthalimide
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A mild and efficient method for the synthesis of 5-substituted isoxazoles through cyclization of propargylic amines with N-hydroxyphthalimide (NHPI) under metal-free conditions was developed.
- Zhang, Yicheng,Chen, Wei,Jia, Xueshun
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supporting information
p. 2181 - 2183
(2018/05/08)
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- TEMPO-catalyzed synthesis of 5-substituted isoxazoles from propargylic ketones and TMSN3
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A novel and efficient TEMPO-catalyzed synthesis of 5-substituted isoxazoles from propargylic ketones and TMSN3via a radical mechanism process is described. This methodology provides an easy access to a variety of useful 5-substituted isoxazoles
- He, Yan,Xie, Yu-Yang,Wang, Ying-Chun,Bin, Xiao-Min,Hu, Da-Chao,Wang, Heng-Shan,Pan, Ying-Ming
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p. 58988 - 58993
(2016/07/06)
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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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- An efficient synthesis of isoxazoles and pyrazoles under ultrasound irradiation
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A series of 5-arylisoxazole and 5-aryl-1H-pyrazole derivatives was synthesized by the reaction of 3-(dimethylamino)-1-arylprop-2-en-1-one with hydroxylamine hydrochloride or hydrazine hydrate under ultrasound irradiation without using any catalyst. This m
- Huang, Zhi-Bin,Li, Li-Li,Zhao, Yan-Wei,Wang, Hui-Yuan,Shi, Da-Qing
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p. E309-E313
(2014/11/07)
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- Clean and efficient synthesis of isoxazole derivatives in aqueous media
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A series of 5-arylisoxazole derivatives were synthesized via the reaction of 3-(dimethyl-amino)-1-arylprop-2-en-1-ones with hydroxylamine hydrochloride in aqueous media without using any catalyst. This method has the advantages of easier work-up, mild rea
- Dou, Guolan,Xu, Pan,Li, Qiang,Xi, Yukun,Huang, Zhibin,Shi, Daqing
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p. 13645 - 13653
(2014/01/06)
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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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- Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands
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A several series of low molecular weight 5-HT2A leads were identified from an analysis of HTS data, the exploration of SAR and optimization of one series using parallel synthesis are described, affording compound 22 (5-HT2A IC50 1.1 nM).
- Swain, Christopher J.,Teran, Ana,Maroto, Marta,Cabello, Angeles
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p. 6058 - 6062
(2007/10/03)
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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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- New Synthesis of Pyrazole and Isoxazole Derivatives
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A convenient synthesis of 5-aryl-1-phenylpyrazoles and 5-arylisoxazoles, from readily available ketimine 1 dimethylformamide dimethylacetal and phenylhydrazine or hydroxylamine, is described.
- Molina, P.,Fresneda, P. M.
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p. 461 - 464
(2007/10/02)
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- New Synthesis of Isoxazoles and Isothiazoles. A Convenient Synthesis of Thioenaminones from Enaminones
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The reaction of 1-aryl-3-(dimethylamino)-2-propene-1-ones (enaminones) and 1-aryl-3-(dimethylamino)-2-propene-1-thiones (thioenaminones) with hydroxylamine-O-sulfonic acid gave, respectively, isoxazoles in 76-84 percent yields and isothiazoles in 60-65 pe
- Lin, Yang-i,Lang, Stanley, A.
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p. 4857 - 4860
(2007/10/02)
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