Chiral separation and preparation of three new antagonists of alpha 1-adrenoceptors by chiral mobile phase HPLC / 药学学报

ABSTRACT

<p><b>AIM</b>To establish new methods for the chiral separation and preparation of three new drugs, alfuzosin, terazosin and doxazosin.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>The enantiomers of three new drugs were base-line-separated and milligram-scale samples of enantiomer were obtained.</p><p><b>CONCLUSION</b>The newly established method can be used in research and development of the enantiomers of three new drugs.</p>