- 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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- An efficient solvent-free synthesis of isoxazolyl-1,4-dihydropyridines on solid support SiO2 under microwave irradiation
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An efficient synthesis of 1,4-dihydropyridines was developed. 1,4-Dihydropyridines were synthesized starting from various 3-substituted isoxazolyl-5-carbaldehydes, ethyl acetoacetate, and ammonium acetate under microwave irradiation and solvent-free conditions (86–96?%), and were characterized by HRMS, FT-IR, 1H NMR, and 13C NMR spectroscopy. Solid support SiO2 was found to possess favorable catalysis and dispersancy for the condensation reaction. The merits of the method included the environmental friendly reaction conditions, simple operation, extensive substrates, good yields and reuse of the SiO2. Moreover, the crystal structure of compound diethyl 4-[3-(2-methoxyphenyl)isoxazol-5-yl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate in orthorhombic Pbca space group was presented. Graphical abstract: [Figure not available: see fulltext.]
- Zhang, Dawei,Chen, Xiaodong,Guo, Xue,Zhang, Yumin,Hou, Yaya,Zhao, Tianqi,Gu, Qiang
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p. 1605 - 1614
(2016/08/16)
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- ISOXAZOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of isoxazole containing compounds are disclosed of the general formula (1) where Z is N or CHNR3 and (Ar1)2CR4 is optionally substituted benzhydryl.
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Page/Page column 26-27
(2008/06/13)
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- Synthesis and biological evaluation of novel T-type Ca2+ channel blockers
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A small molecule library of piperazinylalkylisoxazole derivatives containing about 600 compounds was designed, synthesized and evaluated for blocking effects on T-type Ca2+ channel. Several ligands were identified to possess high inhibitory activity against the T-type Ca 2+ channel. The compound 21 with trifluoromethyl substituents at C3-position of phenyl group (R1) and C2- position of phenyl group (R2) showed the highest inhibitory activity with IC50 value of 1.02μM, which is comparable to that of mibefradil.
- Jung, Hee Kyung,Doddareddy, Munikumar Reddy,Cha, Joo Hwan,Rhim, Hyewhon,Cho, Yong Seo,Koh, Hun Yeong,Jung, Bong Young,Pae, Ae Nim
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p. 3965 - 3970
(2007/10/03)
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