【摘要】 采用自制高活性面包酵母细胞不对称生物还原3-氯代苯丙酮合成高纯度(S)-(-)-3-氯-1-苯基-1-丙醇,考查了pH值、温度、反应时间、有氧无氧对反应产率和对映体过量值的影响。然后与甲胺和1-氯-4-三氟甲基苯反应制备(S)-盐酸氟西汀。结果表明,合成(S)-(-)-3-氯-1-苯基-1-丙醇的最佳工艺条件为:在无氧环境下,在pH值为7的500mL缓冲溶液中,加入3-氯代苯丙酮1.5g,D-葡萄糖30g,活化酵母30g和6mL乙醇,在23℃反应63h,最终产率为61.3%,对映体过量值大于99%。(S)-盐酸氟西汀的总收率约为61.7%(以(S)-(-)-3-氯-1-苯基-1-丙醇计)。更多还原

【Abstract】 (S)-(-)-3-Chloro-1-phenyl-propanol was synthesized by asymmetric bioredution with highly active bread yeast cells for 3-chloropropiophenone.The method of extraction and purification and bioreduction condition were improved.The effects of pH value,temperature,reaction time and anaerobic or aerobic circumstance on the yield and the enantiometric excess of the product were evaluated.(S)-fluoxetine hydrochloride was synthesized with(S)-(-)-3-chloro-1-phenyl-propanol,methylamine and 1-chloro-4-benzotrifluoride.Under the optimum biotransformation condition,the reaction field of (S)-(-)-3-chloro-1-phenyl-1-propanol was 61.3%,and the enantiomeric excess value was more than 99.6%.The overall yield of (S)-fluoxetine hydrochloride was about 61.7%(based on (S)-(-)-3-chloro-1-phenyl-1-propanol).更多还原