Convergent synthesis was developed to prepare both enantiomers of propargyl alcohols for enantio-selective synthesis of a novel thrombin receptor antagonist Sch530348 and its analogs. This method employs kinetic resolution of a rac-propargyl alcohol by a lipase, followed by the inversion of the antipode through its tosylate. All the steps were carried out in one stream. This method was demonstrated by preparing both (R) and (S) enantiomers from a racemic alcohol on multi-gram scale.