【摘要】 利用铁基手性络合催化剂Fe Cl2(TPP)2[(1S,2S)-DPEN]/-γ-Al2O3对3-氯-1-(2-噻吩)丙酮进行催化加氢而制得抗抑郁药度洛西汀中间体(S)-3-氯-1-(2-噻吩)丙醇,与以往的方法相比,此方法不仅产率高且绿色环保。并探讨了温度、氢压和加氢时间对产物转化率以及选择性的影响。实验结果表明:温度在25℃,氢压在1.2MPa,反应时间在10h,3-氯-1-(2-噻吩)丙酮的转化率98%,(S)-3-氯-1-(2-噻吩)丙醇的e.e值为85%。更多还原

【Abstract】 For the synthesis of the antidepressant duloxetine intermediate(S)-3- chloro-1-(2-thienyl)propanol, a more efficient and environment protecting way has been developed through catalytic hydrogenation of3-chloro-1-(2-thienyl)acetone in the presence of a chiralcomplexiron-basedcatalyst supported on Al2O3. The effects of reaction temperature, hydrogen pressure, time of hydrogenation on the conversion rate and the product se-lectivity have been studied. The results show that when the temperature is 25℃ and the hydrogen pressure is 1.2MPa, the conversion?rate of 3-chloro-1-(2-thienyl)acetone is 98% and the e.e.% of(S)-3- chloro-1-(2-thienyl)propanol is 85% in ten hours.更多还原