摘要:
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.
Abstract:
Objective To optimize the preparation procedure of aripiprazole. Methods 7-hydroxy-3,4-dihydro-2(1H)-quinolin-one was used as starting material and etherified with 1,4-dibromobutane, then alkylated with 1-(2,3-dichlorophenyl) piperazine to yield the target compound aripiprazole. Results The DMF was replaced by acetone as solvent when etherification. The extraction purification method in the last step was replaced by washing precipitates with water. Aripiprazole was prepared in overall yield of 71. 3%. Conclusion The optimal preparation procedure is stable and available for industrial production.
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