Abstract <p>A reproducible and scalable method for the synthesis of promising tuberculostatic agents—<i>N</i>-acylhydrazono podands—in water without the use of catalysts has been developed. The effect of the molar ratios of the starting reagents and the solvent (ethanol or water), as well as the duration of ultrasonic irradiation, on the yield of the target product was studied. The increased selectivity of the condensation reaction of formyl podands with isoniazid in water under ultrasonic irradiation provides an almost quantitative yield of the target products without additional purification. The method can be recommended for the synthesis of a wide range of pharmacologically significant substituted hydrazones.</p>

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Green Method for the Synthesis of Promising Tuberculostatic Agents—N-Acylhydrazono Podands—in Water

  • Olga V. Fedorova,
  • Irina G. Ovchinnikova,
  • Pavel A. Slepukhin,
  • Gennady L. Rusinov

摘要

Abstract

A reproducible and scalable method for the synthesis of promising tuberculostatic agents—N-acylhydrazono podands—in water without the use of catalysts has been developed. The effect of the molar ratios of the starting reagents and the solvent (ethanol or water), as well as the duration of ultrasonic irradiation, on the yield of the target product was studied. The increased selectivity of the condensation reaction of formyl podands with isoniazid in water under ultrasonic irradiation provides an almost quantitative yield of the target products without additional purification. The method can be recommended for the synthesis of a wide range of pharmacologically significant substituted hydrazones.