Synthetic route optimization of Sumepirin antiepileptic drug candidate

M. S. Dzyurkevich; N. V. Shtyrlin; Y. G. Shtyrlin

doi:10.15826/chimtech.2020.7.4.04

Synthetic route optimization of Sumepirin antiepileptic drug candidate

M. S. Dzyurkevich, N. V. Shtyrlin, Y. G. Shtyrlin

Abstract

In this work we describe the transformation of synthetic route of the antiepileptic drug candidate Sumepirin starting from discovery stage. Initial method included six step process requiring two steps of purification using colon chromatography and has poor overall yield of target compound. The process developed is convenient, scalable, technological and meet the most of conditions of green chemistry. The overall yield was increased up to 62.5% in four steps without colon chromatography purification which allows to obtain the target compound with purity of 99.5+% which is especially important for the active ingredient.

Keywords

pyridoxine; synthetic route optimization; scale-up; purification; antiepileptic drug; technology

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DOI: https://doi.org/10.15826/chimtech.2020.7.4.04

Copyright (c) 2020 M. S. Dzyurkevich, N. V. Shtyrlin, Y. G. Shtyrlin

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