title: Preparative enantioseparation of propafenone by counter-current chromatography using di-n-butyl L-tartrate combined with boric acid as the chiral selector.
abstract: This paper extends the research of the utilization of borate coordination complexes in chiral separation by counter-current chromatography (CCC). Racemic propafenone was successfully enantioseparated by CCC with di-n-butyl l-tartrate combined with boric acid as the chiral selector. The two-phase solvent system was composed of chloroform/ 0.05 mol/L acetate buffer pH 3.4 containing 0.10 mol/L boric acid (1:1, v/v), in which 0.10 mol/L di-n-butyl l-tartrate was added in the organic phase. The influence of factors in the enantioseparation of propafenone were investigated and optimized. A total of 92 mg of racemic propafenone was completely enantioseparated using high-speed CCC in a single run, yielding 40-42 mg of (R)- and (S)-propafenone enantiomers with an HPLC purity over 90-95%. The recovery for propafenone enantiomers from fractions of CCC was in the range of 85-90%.
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, P. R. China.
authors.forename: Shengqiang
authors.initials: S
authors.lastname: Tong
authors.forename: Mangmang
authors.initials: M
authors.lastname: Shen
authors.forename: Ye
authors.initials: Y
authors.lastname: Zheng
authors.forename: Chu
authors.initials: C
authors.lastname: Chu
authors.forename: Xing-Nuo
authors.initials: XN
authors.lastname: Li
authors.forename: Jizhong
authors.initials: J
authors.lastname: Yan
mesh_terms: D001888:Boric Acids / Q000737:chemistry*; D003377:Countercurrent Distribution; D059625:Liquid-Liquid Extraction; D015394:Molecular Structure; D011405:Propafenone / Q000737:chemistry / Q000302:isolation & purification*; D013237:Stereoisomerism; D013644:Tartrates / Q000737:chemistry*
chemical_list: D001888:Boric Acids; D013644:Tartrates; D011405:Propafenone; C032688:boric acid
keywords: Boric acid; Chiral separation; Counter-current chromatography; Di-n-butyl l-tartrate; Propafenone