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目的合成(S)-氯吡咯雷的关键中间体——(R)-(-)邻氯扁桃酸甲酯,并建立了优化的还原条件。方法以邻氯苯乙酮酸甲酯为底物,利用酵母菌DM10的醇脱氢酶及其辅酶合成(R)-(-)邻氯扁桃酸甲酯,并考察了底物质量浓度、初始pH、转化温度和反应时间对不对称还原的影响。结果和结论获得优化的还原条件:接种量体积分数为10%,初始pH值为6.5,底物质量浓度为1 g.L-1,温度为30℃,转化36 h,转化率为98.75%,产率为82.25%,对映体过量值为95.1%。
Aim To synthesize methyl (-) - o-chloromandelate, a key intermediate of (S) -chloropyrrole, and optimize the reduction conditions. Methods Methyl (R) - (-) o-chloromandelate was synthesized from o-chlorophenyl methyl ketal using alcohol dehydrogenase and its coenzyme from yeast DM10. The effects of substrate concentration, Effect of pH, Conversion Temperature and Reaction Time on Asymmetric Reduction. RESULTS AND CONCLUSIONS The optimal conditions were as follows: the volume fraction of inoculum was 10%, initial pH was 6.5, substrate concentration was 1 gL-1, temperature was 30 ℃, transformation time was 36 h, conversion rate was 98.75% 82.25%, enantiomeric excess 95.1%.