本文报导利用糖精(甲苯磺酰化法)的副产物对甲苯磺酰氯为原料,先制成对甲苯磺酰胺;然后在碱存在下与二氯乙烷进行缩合生成N,N′-双(对甲苯磺酰)胡椒嗪;再经浓磷酸高温水解成胡椒嗪的酸性磷酸盐;最后经碱中和即得临床上需用的磷酸胡椒嗪一水合物,对于缩合反应的反应时间、配料比例、缩合剂和中和剂的选择,溶剂的影响以及反应后处理的方法等都进行了一些考察. This paper reports the use of saccharin (tosylation method) by-product p-toluenesulfonyl chloride as raw material, first made p-toluenesulfonamide; then in the presence of base with dichloroethane condensation to generate N, N’- Toluenesulfonyl) piperzine; and then hydrolyzed by concentrated phosphoric acid into piperitine acid phosphate; finally, alkali neutralization results in clinically required piperpirin monohydrate, and the reaction time for the condensation reaction, the proportion of ingredients, The choice of condensing agent and neutralizer, the influence of solvent and the method of post-reaction treatment.