- Synthesis of 5-Arylisoxazole and 4,5-Dichloroisothiazole Amino-Substituted Derivatives and Their Biological Activity
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Abstract: A series of amino derivatives of 5-arylisoxazoles and 4,5-dichloroisothiazole with primary and secondary amino groups was synthesized. 3-Aminomethyl-5-arylisoxazol-3-ylmethanamines were obtained on the basis of 5-aryl-3-(chloromethyl)isoxazoles using the Gabriel phthalimide method. 5-Arylisoxazol-3-yl- and 4,5-dichloroisothiazol-3-ylallylamines were synthesized in two ways: reduction of azomethines obtained by condensation of 5-arylisoxazolyl- and 4,5-dichloroisothiazolyl-3-carbaldehydes with allylamine, and by nucleophilic substitution of the chlorine atom in 3-chloromethyl derivatives of the corresponding azoles by reaction with allylamine. Amides and sulfonamides of azolylallylamines were synthesized. Some of the compounds obtained showed antibacterial and fungicidal activity.
- Chervyakova, L. V.,Guan, A. Y.,Kolesnik, I. A.,Liu, C. L.,Mertsalov, D. F.,Nadirova, M. A.,Petkevich, S. K.,Potkin, V. I.,Tyurin, A. P.
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- NOVEL JNK INHIBITORS
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Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0.
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Page/Page column 138; 139
(2008/12/07)
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- Regioselective syntheses of 3-aminomethyl-5-substituted isoxazoles: A facile and chemoselective reduction of azide to amino by sodium borohydride using 1,3-propanedithiol as a catalyst
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A series of isoxazole azides were reduced selectively to isoxazole amines in quantitative yield by sodium borohydride using 1,3-propanedithiol as a catalyst.
- Pei,Wickhan
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p. 7509 - 7512
(2007/10/02)
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