Drug synthesis, separation, and identification of a di-stereoisomeric mixture of spiro-oxalidinonic derivatives of sorbinil by high-performance liquid chromatography

Author:

,Khalfa Esaim FadhelORCID,Abdullah Rawaa G.ORCID, ,Al-Daami Qasim JawadORCID, ,Bash AymenORCID, ,Al-Qaysi Saba Abdulmunem HabeebORCID, ,Jasim Mohammed GhassanORCID, ,Al-Jabbar Mozzan Widad AbdORCID,

Abstract

A straightforward and sensitive method for high-performance liquid chromatography (HPLC) was created in order to separate and identify the di-stereoisomeric mixture of a spiro-oxalidinonic derivative of sorbinil. HPLC was carried out using a C18 reversed-phase column. The mobile phase used in the isocratic elution process was a 70:30 v/v combi¬nation of methanol and acetonitrile flowed at a rate of 2 mL/min. The procedure delivered the best result among the various attempts made. Two peaks were identified on the chromatogram, attributable to the two di-stereoisomers of the mixture analysed. Analogues of sorbinil, a powerful inhibitor of aldose reductase, have been synthesized and further tested on aldose reductase as mixtures of di-stereoisomers, exhibiting an IC50 in the order of the micromolar. The structure of the compounds was checked with nuclear magnetic resonance spectroscopy. The chemical shifts were expressed in ppm scale δ.

Publisher

PHARMAKON-Press

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