报道了(R)-和(S)-磷酸苯丙哌林对映体的合成新方法.以邻苄基苯酚和(S)-(+)-环氧氯丙烷为原料,通过成醚、选择性还原开环两步反应简捷高效地制得重要中间体(R)-1-(2-苄基苯氧基)-2-丙醇(2).中间体2与对甲苯磺酰氯酰化,制得中间体(R)-1-(2-苄基苯氧基)-2-丙醇对甲苯磺酸酯(3),该中间体与哌啶发生一次SN2反应直接得到(S)-(-)-苯丙哌林,该中间体与溴化锂和哌啶发生两次SN2反应制得(R)-(+)-苯丙哌林.然后它们分别与磷酸成盐制得相应的(S)-(-)-和(R)-(+)-磷酸苯丙哌林,其结构通过1H NMR和HRMS进行了表征.该合成方法路线短,反应条件温和,易于操作,且收率好,适合工业化生产. A new method for the synthesis of enantiomers of (R) - and (S) -benproperpirone phosphate has been reported. By using o-benzylphenol and (S) - (+) - epichlorohydrin as starting materials, A simple and efficient method for the preparation of the important intermediate (R) -1- (2-benzylphenoxy) -2-propanol (2) The intermediate (R) -1- (2-benzylphenoxy) -2-propanol p-toluenesulfonate (3) was prepared and this intermediate reacted once with SNP to give (S) (-) - benproperine, which is converted to (R) - (+) - benproperine by two SN2 reactions with lithium bromide and piperidine, which are then salified with phosphoric acid to give the corresponding (S) - (-) - and (R) - (+) - benproperide phosphate and its structure has been characterized by 1H NMR and HRMS.The method has the advantages of short route, mild reaction conditions, easy operation and good yield Industrial production.