PROCESS FOR PREPARATIVE RESOLUTION OF TERBUTALIN ENANTIOMER

摘要

PURPOSE: Provided is a method for manufacturing terbutaline enantiomer from terbutaline racemate in a higher yield than the yield that existing R-(-)-terbutaline asymmetric synthesis and chromatographic chiral separation produce. CONSTITUTION: A method for manufacturing terbutaline enantiomer is comprised of the following steps: i) adding S-(-)-¬-methylbenzyl isocyanate to terbutaline racemate to manufacture ()-diestereomer; ii) separating ()-diestereomer into (+),(-)- diestereomer using ODS in the presence of water and methanol as solvent; and iii) hydrolyzing (+),(-)-diestereomer to obtain and purify terbutaline enantiomer through chromatography. And terbutaline racemate and S-(-)-¬-methylbenzyl isocyanate are mixed in a molar ratio of 1:5.