Research On Chiral Resolution Of Citalopram Enantiomers

In this paper, chiral resolution of citalopram enantiomers was researched. The main contents can be summarized as follows:Enantiomeric separation of citalopram was developed using a reversed phase HPLC (RP-HPLC) with sulfobutylether-β-cyclodextrin (SBE-β-CD) as a chiral mobile phase additive. A new quantitative analytic method of citalopram enantiomers by HPLC was established. The influential factors were investigated, and an optimized condition was obtained. The validity of this method is proven by precision, linearity, limit of detection (LOD) and limit of quantitation (LOQ). The separation mechanism was analyzed through thermodynamics.The optical activs N-carbobenzyloxy-L-alanine (Z-L-Ala) was synthesized using L-alanine (L-Ala) and N-(Benzyloxycarbonyloxy)succinimide (Z-osu) as the raw material. The influential factors were investigated. The structure of compound was characterized by IR,’HNMR and elemental analysis; Using Z-L-Ala as chiral selector in organic phase and SBE-β-CD as chiral selector in aqueous phase, the resolution of citalopram enantiomers in a biphasic recognition extraction system was researched. The influential factors were investigated. The laws of the experiment results were analyzed and the mechanisms were discussed.A new method of crystallization resolution of citalopram enantiomers by forming diastereomeric salt was researched. Using S-(+)-Naproxen> (-)-Dibenzoyl-L-tartaric acid、 R-(-)-Mandelicacid、R-(-)-o-Chloromandelicacid、(S)-(+)-10-Camphorsulfonicacid、and (+)-Di-p-toluoyl-D-tartaric acid (DTTA) as chiral selectors respectively, the research was taken on in different solvents and the experiment results were analyzed.