title: [Chiral separation and preparation of three new antagonists of alpha 1-adrenoceptors by chiral mobile phase HPLC].
abstract: OBJECTIVE
  To establish new methods for the chiral separation and preparation of three new drugs, alfuzosin, terazosin and doxazosin.
  
  
  METHODS
  By optimizing factors which affect the chiral separation, modifier of solvent, chiral additive, pH of mobile phase, modifier of organic base and stationary phase, the optimum condition for chiral separation were selected. The preparation of enantiomers was carried out on semi-preparative reverse phase column (7.8 mm x 250 mm C4 5 microns). Acetonitrile-water modified by the addition of carboxymethyl-beta-cyclodextrin (2%-5%, w/v) was applied as chiral mobile phase.
  
  
  RESULTS
  The enantiomers of three new drugs were base-line-separated and milligram-scale samples of enantiomer were obtained.
  
  
  CONCLUSIONS
  The newly established method can be used in research and development of the enantiomers of three new drugs.
authors.affiliation: Department of Pharmacology, School of Pharmacy, Hebei Medical University, Research and Development Drug Center, North China Pharmaceutical Corporation, Shijiazhuang, China. niuchangqun@yeal.net
authors.forename: Chang-qun
authors.initials: CQ
authors.lastname: Niu
authors.forename: Lei-ming
authors.initials: LM
authors.lastname: Ren
mesh_terms: D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000302:isolation & purification*; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D017292:Doxazosin / Q000302:isolation & purification; D015394:Molecular Structure; D011224:Prazosin / Q000031:analogs & derivatives* / Q000302:isolation & purification; D011799:Quinazolines / Q000302:isolation & purification
chemical_list: D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D011799:Quinazolines; C041226:Terazosin; C047638:alfuzosin; D017292:Doxazosin; D011224:Prazosin