DOI: https://doi.org/10.15587/2519-4852.2016.87441

Technology scaling for obtaining N,N –dibenzyl amide of malonic acid – a potential anticonvulsant – in industrial environments

Василь Миколайович Кушнірук, Інна В’ячеславівна Ковалевська, Олена Анатоліївна Рубан, Наталія Василівна Гарна, Вікторія Акопівна Георгіянц

Abstract


In result of a targeted synthesis, a promising substance for new anticonvulsant drug creation – symmetrical dybenzyl amid of malonic acid – was found.

The ability to be synthesized in one stage from available reagents and with high yield, as well as to show in animal experiments anticonvulsant activity with low toxicity is specific for the given substance.

The aim of our research was to determine optimal conditions for synthesis of N,N- dybenzyl amid of malonic acid and to scale the method in industrial production.

Methods. N,N- dybenzyl amid of malonic acid was obtained by synthesis. Purity was estimated using chromatographic methods. Crystals microscopy was carried out for study physical and chemical properties of the synthesized dybenzyl amid of malonic acid.

Results. In result of research, the method of N,N- dybenzyl amid of malonic acid synthesis was elaborated under manufacturing conditions; the influence of the  reaction latency and reagents ratio on the product yield was studied.

Conclusion. The method of N,N- dybenzyl amid of malonic acid synthesis was elaborated under manufacturing conditions considering modern requirements to the active pharmaceutical ingredients quality and safety. The choice of the initial substances, solvent, synthesis and purification conditions was substantiated to ensure the final product’s appropriate purity and high yield.

The obtained results can be used for N,N- dybenzyl amid of malonic acid synthesis in industrial environments

Keywords


synthesis; N;N-dybenzyl amid of malonic acid; anticonvulsant activity; reaction latency; reagents ratio

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GOST Style Citations


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