目的:优化阿立哌唑的制备工艺。方法:以7-羟基-3,4-二氢-2-(1H)-喹啉酮为起始原料,经与1,4-二溴丁烷醚化后,再与1-(2,3-二氯苯基)哌嗪缩合,制得阿立哌唑。结果:醚化时用丙酮替代DMF作溶剂,反应副产物减少;由中间体Ⅲ制备终产物Ⅰ原工艺采用萃取法纯化,溶剂消耗多,成本高,本文中改由直接大量多次水洗产品,操作简便,产物纯度符合要求,总收率达到71.3%。结论:优化后的制备工艺稳定可行,适合工业化生产要求。 Objective: To optimize the preparation process of aripiprazole. Methods: Starting from 7-hydroxy-3,4-dihydro-2- (1H) -quinolinone and etherification with 1,4-dibromobutane, - dichlorophenyl) piperazine condensation, the aripiprazole. Results: The etherification process was replaced by acetone instead of DMF, and the reaction by-products decreased. The final product I was prepared from intermediate Ⅲ. The original process was purified by extraction method, the solvent consumption was high and the cost was high. In this paper, Easy operation, product purity to meet the requirements, the total yield reached 71.3%. Conclusion: The optimized preparation process is stable and feasible, suitable for industrial production requirements.