SELECTIVE PREPARATION METHOD OF (+)-CIS-SERTALINE WITH HIGH OPTICAL PURITY WITHOUT ADDITIONAL PURIFICATION BY USING (S)-(-)-2-PYRROLIDONE-5-CARBOXYLIC ACID, AS AN OPTICAL DIVIDING AGENT

摘要

PURPOSE: A manufacturing method of a (+)-cis-sertaline is provided to manufacture (+)-cis-sertaline of high purity and high yield which does not includes dechlorinated sertaline byproduct, by selectively separating and purifying only a (+)-cis-sertaline.;CONSTITUTION: A manufacturing method of a (±)-cis-sertaline represented by chemical formula 1 comprises: a step of manufacturing (+)-cis-sertaline (S)-(-)-2-pyrrolidone-5-carboxylate by reaction of (±)-cis/trans-sertaline represented by chemical formula 2 or (±)-cis-sertaline and (S)-(-)-2-pyrrolidone-5-carboxylate and optically dividing the product. The use amount of the (S)-(-)-2-pyrrolidone-5-carboxylate is 0.25-1.0 molar equivalent, based on 0.25-1.0 molar equivalent. The reaction solvent is selected from toluene, ethylacetate, acetone, and ethanol.;COPYRIGHT KIPO 2013