FIELD: chemistry.
SUBSTANCE: invention relates to a method of producing 5-substituted 1,2,4-triazole-3-carboxylic acids and derivatives thereof, involving synthesis of key intermediates - β-Ν-tertbutyloxycarbonyl-alkoxycarbonylamidrazones by reacting tretbutyloxycarbonylhydrazine with equimolar amounts of esters of thiooxamic acid in ethyl alcohol, subsequent acylation of key intermediate with acyl chlorides of carboxylic acids in pyridine without extraction of reaction product - N-acylated N-Boc amidrazone and its cyclisation in pyridine while boiling, followed by extraction of obtained derivatives of 5-substituted 1,2,4-triazole-3-carboxylic acids by extraction, recrystallisation from organic solvents, such as ethers or halocarbons, or by column chromatography.
EFFECT: technical result is invention provides fewer process steps of obtaining derivatives of 5-substituted-1,2,4-triazole-3-carboxylic acids and higher total output of desired compounds.
1 cl, 3 ex
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Authors
Dates
2016-12-20—Published
2015-11-10—Filed