药物中间体(R)-苄基缩水甘油醚的生物法制备研究

Study on Enzymatic Preparation of (R)-Benzyl Glycidyl Ether

为获得手性苄基缩水甘油醚,以苄基缩水甘油醚为唯一碳源,从土壤中筛选到一株能对映选择性水解拆分苄基缩水甘油醚,获得相应(R)-对映体的菌株,经鉴定为白曲霉,命名为Aspergillus candidus ZJUTZQ041。并利用其冻干细胞,对苄基缩水甘油醚的生物催化拆分进行了研究,最终确定在30℃,磷酸钾缓冲液pH7.6,细胞与底物比为9∶1,助溶剂为二甲基亚砜条件下转化12 h,剩余R型底物的e.e.s值能从62.7%提高到94.7%。

A strain called Aspergillus niger ZJUTZQ041,which was isolated from soil,was investigated for the resolution of racemic benzyl glycidyl ether(BGE)to get the corresponding(R)-BGE.The ee value of the(R)-enantiomer was increased from 62.7% to 94.7% under optimized conditions as follows:30℃,phosphate buffer(100 mM,pH 7.6),cell/substrate ratio 9∶1 and reaction time 12 h.