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GRAPHICAL ABSTRACT
ABSTRACT
Two amino acid phosphoramidates with high antiviral activity were used as model compounds and separated using supercritical fluid chromatography on an achiral Hypersil BDS cyano column (250 × 4.6 mm, 5 µm). Supercritical CO2 was used as a mobile phase with different co-solvents, including methanol, ethanol, and 2-propanol. Several key processing parameters were evaluated, including the type and concentration of alcohol modifier (5 to 15%), backpressure (100 to 200 bar), and column temperature (30 to 45 ˚C) in terms of their impact on retention factor, diastereoselectivity, and resolution. The optimized chromatographic conditions allowed for a complete separation of mixture of two diastereomers with good resolution over a short time (5–9 min). At a backpressure of 150 bar and a temperature of 33°C, the diastereomers of phenylalanine methyl ester phenyl 5′-phosphoamidate of d4T (d4T-P-N-PheOMe) and alanine methyl ester phenyl 5′-phosphoamidate of d4T (d4T-P-N-AlaOMe) were separated with resolutions of 4.43 and 2.55 using 10.0% and 5.0% (v/v) methanol, respectively.
Funding
This study was supported by the National Natural Science Foundation of China (grant Nos. 21232005 and 21375113).