FIELD: organic chemistry, chemical technology.
SUBSTANCE: invention elates to a novel method for synthesis of derivatives of 3-hydroxypyridine. Invention describes a method for synthesis of compound of the formula: wherein R1 and R2 mean independently hydrogen atom, (C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, amino-(C1-C4)-alkyl, (C1-C4)-alkoxy group, carboxy-(C1-C4)-alkyl, trifluoromethyl, thio-(C1-C4)-alkyl, aromatic group optionally substituted with at least one substitute chosen from group comprising (C1-C4)-alkyl, (C1-C4)-alkoxy group, halogen atom and/or trifluoromethyl-substituted phenyl, hydroxyl, hydroxy-(C1-C4)-alkyl, (C2-C4)-alkenyl, (C2-C4)-alkynyl, amino group, (C1-C4)-alkylamino group. Method involves treatment of 2-acylfuran with nitrogen-containing compound of the formula (I): at temperature 130-300°C, under elevated pressure in medium of aqueous or alcoholic ammonia, and wherein in the formula (I) X means NH-group or oxygen atom; R1 means hydrogen atom, (C1-C4)-alkyl, amino group, amino-(C1-C4)-alkyl, (C1-C4)-alkylamino group, hydroxy-(C1-C4)-alkyl; R2 means hydrogen atom or (C1-C4)-alkyl; R3 means hydrogen atom or (C1-C4)-alkyl; R4 means hydrogen atom, (C1-C4)-alkyl, amidated carboxy group. Invention provides increasing yield of the end product, decreasing amount of waste formed during the reaction, and significant rise of economy indices.
EFFECT: improved method of synthesis.
5 cl, 4 ex
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Authors
Dates
2008-03-20—Published
2007-01-19—Filed