NOVEL CHIRAL SANGER'S REAGENTS AND CHROMATOGRAPHIC ENANTIOSEPARATION OF A SERIES OF RACEMIC ß-BLOCKERS AND DFT OPTIMISATION
An effective and sensitive enantioseparation method was developed to identify the enantiomeric purity of racemic- blockers. Followed by the substitution, alkylation and acylation, three novel chiral Sanger’s reagents weresynthesised and characterised with spectroscopic instruments, such as NMR, FT-IR, UV, HRMS and elemental analyser. The diastereomerisation of the -blockers, a racemic beta receptor blocker drug, was carried out usingtheactive Sanger's reagents. RP-HPLC was then used to perform chromatographic separation on the synthesiseddiastereomeric pairs. Analysis was done using the eluting phase, which comprises a Methyl nitrile-based buffer solution. In the presence of multiple variables like pH, concentration, and eluting phase ratio, the separation analysisfindings were optimised. Additionally, through generating minimised energy structures of the prepareddiastereomeric pairings using Gaussian software, the separation procedure, elution sequence, and stable conformer of diastereomeric derivatives were investigated. Validation parameters were determined, and the validationwascarried out in accordance with ICH guidelines.
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