A validated chiral LC method for enantiomeric separation of common intermediate of ritonavir and lopinavir using cellulose based chiral stationary phase

A.Nageswari, P.Surya Prakash R

Abstract

A rapid isocratic chiral LCmethod has been developed for the separation of (2R,3R,5R)-2-Amino-3-hydroxy-5-(tert-butyl oxy carbonyl) amino-1,6-diphenyl hemi succinic acid (R-BOCamine) from(2S,3S,5S)-2-Amino-3-hydroxy- 5-(tert-butyl oxy carbonyl) amino-1,6-diphenyl hemi succinic acid (S-BOC amine). Good resolution with RS > 3 was obtained using cellulose based chiral stationary phase, chiralcelOD-H column (250 x 4.6mm, 5µm particle size) and n-hexane, ethanol, trifluoroacetic acid and triethyl amine (950:50:1:1,v/v) as themobile phase at ambient temperature. Flowrate was kept at 1.0 mLmin-1 and elution wasmonitored by UV detection at 210 nm. This method allowed for the detection and quantification of R-BOC amine of levels at 0.15 and 0.5 µg mL-1 respectively. Themethod was validated by following ICH guidelines.