- A rapid and efficient solvent-free microwave-assisted synthesis of pyrazolone derivatives containing substituted isoxazole ring
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An efficient synthesis of 4-substituted pyrazolone derivatives was developed. 4-Substituted pyrazolone derivatives were synthesized in 78-97% yields starting from various 3-substituted isoxazole-5-carbaldehydes, ethyl acetoacetate and hydrazine under micr
- Zhang, Dawei,Zhang, Yumin,Zhao, Tianqi,Li, Jing,Hou, Yaya,Gu, Qiang
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p. 2979 - 2987
(2016/05/19)
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- Efficient solvent-free synthesis of bis(indolyl)methanes on SiO2 solid support under microwave irradiation
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An efficient synthesis of bis(indolyl)methanes was developed. Bis(indolyl)methanes were synthesized starting from various aromatic aldehydes with indole under microwave irradiation and solvent-free conditions (85-98 %). Solid support SiO2 was found to possess favorable catalytic and dispersancy parameters for the condensation reaction. Moreover, novel bis(indolyl)methanes containing an isoxazole ring were synthesized via this method in excellent yields (> 94 %) using 3-substituted isoxazole-5-carbaldehydes and indole.
- Zhang, Da-Wei,Zhang, Yu-Min,Zhang, Yi-Liang,Zhao, Tian-Qi,Liu, Hong-Wei,Gan, Yuan-Ming,Gu, Qiang
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p. 470 - 478
(2015/01/30)
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- Synthesis of novel 5-(3-alkylquinolin-2-yl)-3-aryl isoxazole derivatives and their cytotoxic activity
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The propargyl alcohol on reaction with aldoxime and NaOCl in DCM gave exclusively (3-arylisoxazol-5-yl) methanol 1. The compound 1 was oxidized to an aldehyde 2 followed by reaction with aniline resulted in Schiff's base 3. The compounds 3 were further re
- Sambasiva Rao,Kurumurthy,Veeraswamy,Poornachandra,Ganesh Kumar,Narsaiah
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supporting information
p. 1349 - 1351
(2014/03/21)
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- GLYCINE TRANSPORTER INHIBITING SUBSTANCES
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The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, pain, and sleep disorder:
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Paragraph 0438; 0441; 0446
(2013/07/25)
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- Synthesis and preliminary antibacterial evaluation of 2-butyl succinate-based hydroxamate derivatives containing isoxazole rings
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Two series of novel 2-butyl succinate-based Hydroxamate derivatives containing isoxazole rings were synthesized, characterized and evaluated for antibacterial activity. The synthesized compounds were found to exhibit weak to moderate inhibitory activity against Staphytlococcus aureu and Klebsiellar pneumonia in vitro. All the compounds synthesized were found to be more effective against Klebsiellar pneumonia compared to Staphytlococcus aureu.
- Zhang, Datong,Jia, Jiong,Meng, Lijuan,Xu, Weiren,Tang, Lida,Wang, Jianwu
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p. 831 - 842
(2012/01/04)
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- PIPERIDINE-CONTAINING COMPOUNDS AND USE THEREOF
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A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I) wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.
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Page/Page column 108
(2010/08/04)
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- Construction of two vicinal quaternary carbons by asymmetric allylic alkylation: Total synthesis of hyperolactone C and (-)-biyouyanagin A
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Call on triple A: Palladium-catalyzed asymmetric allylic alkylation (Pd-AAA; see scheme) has enabled a concise and efficient synthesis of hyperolacto ne C and (-)-biyouyanagin A in only six (20% Overall yield) and seven (8% overall yield) steps, respectively. The enantiomers of these natural products were also prepared by exploiting the same methodology.
- Du, Chao,Li, Liqi,Li, Ying,Xie, Zhixiang
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supporting information; experimental part
p. 7853 - 7856
(2010/04/05)
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- Efficient access to isoxazoles from alkenes
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The direct regioselective synthesis of 3,5-disubstituted isoxazoles was achieved in one reaction vessel through a sequence of reactions involving the net bromination of an electron-deficient alkene, in situ generation of a nitrile oxide, 1,3-dipolar cycloaddition, and loss of HBr from an intermediate 5,5-disubstituted bromoisoxazoline. This one-pot process enables the synthesis of 3,5-disubstituted isoxazoles directly from electron-deficient alkenes thereby negating the isolation of the 1,1-disubstituted bromoalkene alkyne surrogate. Georg Thieme Verlag Stuttgart.
- Xu, Jianping,Hamme II, Ashton T.
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p. 919 - 923
(2008/12/22)
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