FIELD: organic chemistry. SUBSTANCE: product: 4-acetyl-5-para-iodophenyl-1- carboxymethyl-3-hydroxy-2,5-dihydropyrrol of the formula . Synthesis is carried out by interaction of acetylpyruvic acid methyl ester, glycocol and p-iodobenzaldehyde at room temperature by the following scheme: . Yield is 71%, m. p. is 286-288 C (at decomposition). Found, %: C - 41.80; H - 3.00; N - 3.45; J - 31.60; empirical formula is C14H12NO2I. Calculated, %: C - 41.87; H - 3.01; N - 3.49; J - 31.65. Analgetic activity of compound exceeds that of compound-analog and standard by 35.4 and 2 time, respectively. Toxicity of compound is 2500 mg/kg that by 2-fold and 6.6-fold less as compared with that of analog and ortophen, respectively. EFFECT: enhanced analgetic activity, increased yield.
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Authors
Dates
1996-10-10—Published
1994-07-27—Filed