帕罗西汀中间体还原反应工艺研究

Study on the Reduction Reaction Process of Paroxetine Intermediate

研究了硼氢化钠-甲醇-叔丁醇体系将帕罗西汀中间体(4-(4-氟苯基)-3-乙氧羰基-1-甲基哌啶-2,6-二酮)进行还原的反应,分别考察了还原催化体系、温度和投料比等条件对反应收率的影响。结果表明,以叔丁醇作溶剂,甲醇做催化剂,原料二酮、硼氢化钠的摩尔比为1:5.5,反应温度50℃下反应2 h,收率88%。该工艺具有收率较高、工艺简单和环境友好等特点,具有较好的产业化应用前景。

The paroxetine intermediate(4-(4-fluorophenyl)-3-ethoxy-1-methylpiperidine-2,6-dione) was reduced by the catalytic system of sodium borohydride-methanol-t-butyl alcohol. Then, the effect of reduction reaction conditions such as reduction catalysts system, temperature and feed ratio on the reaction yield were mainly discussed. The results showed that 88% yield of product was gotten in 2 h, with t-butyl alcohol as solvent, methanol as co-catalyst, the molar to its advantages such as good yield, simple process, and environmental friendly. ratio of raw material dione and sodium borohydride was 1:5.5, and the reaction temperature was 50℃.The progress has better prospect for industrial application due.