组合拆分法制备米那普仑(1S,2R)对映体

摘要

Objective Using combinatorial resolution to prepare dextrogyral enantiomer of milnacipran(1S,2R). Methods Using the method of combinatorial resolution, the split reagent is one of the resolving reagent family T1: D-(+)-DTTA and D-(+)-DATA, the split solvent is acetone-water(98:2, V/V), the enantiomeric purities was determined by the Chiral-AGP column. Results Succeed preparation milnacipran(1S,2R), yield 80%, enantiomeric excess of milnacipran(1S,2R) was over 98.0%. Conclusion Using combinatorial resolution can get good yield and purity milnacipran(1S,2R).%目的 用组合拆分法制备米那普仑(1S,2R)对映体；方法 通过组合拆分的方法,以光学活性的酒石酸衍生物组成的拆分剂族为拆分试剂,丙酮-水(98∶2,V/V)为拆分溶剂,并采用Chiral-AGP手性柱对产品进行了检测；结果 成功制备了米那普仑(1S,2R)对映体,拆分收率达80％,光学纯度e.e.值大于98.0％;结论 用组合拆分法可以得到较为理想收率和纯度的(1S,2R)米那普仑.