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发明公开
CN110759885A 制备光活依格鲁特的方法 有权

制备光活依格鲁特的方法
摘要：
本发明涉及利用成盐及拆分的方法从式(I)所示N-[2-(2,3-二氢-1,4-苯并二噁烷基-6-基)-2-羟基-1-(1-吡咯烷基甲基)乙基)]辛酰胺四个立体异构体中拆分得到具有单一光学活性的如式(III)所示的N-[(1R,2R)-2-(2,3-二氢-1,4-苯并二噁烷基-6-基)-2-羟基-1-(1-吡咯烷基甲基)乙基)]辛酰胺的方法,再通过酒石酸衍生物或者4-羟基二萘并[2,1-D:1′,2′-F][1,3,2]二磷杂庚英-4-氧化物及其衍生物，特别是D-(+)-二对甲基苯甲酰酒石酸以及(-)-4-羟基二萘并[2,1-D:1′,2′-F][1,3,2]二磷杂庚英-4-氧化物，作为拆分剂，通过旋光拆分，从对映体(RR,SS)N-[2-(2,3-二氢-1,4-苯并二噁烷基-6-基)-2-羟基-1-(1-吡咯烷基甲基)乙基)]辛酰胺中分离得到N-[(1R,2R)-2-(2,3-二氢-1,4-苯并二噁烷基-6-基)-2-羟基-1-(1-吡咯烷基甲基)乙基)]辛酰胺的方法。
摘要（英）：

The invention relates to a method for preparing N-[(1R,2R)-2-(2,3-dihydrogen-1,4-benzodioxyl-6-yl)-2-hydroxyl-1-(1-pyrrolidyl methyl) ethyl] octanamide which has single optical activity and is of a formula (III) shown in the description by resolving four stereisomers of N-[2-(2,3-dihydrogen-1,4-benzodialkyl-6-yl)-2-hydroxyl-1-(1-pyrrolidyl methyl) ethyl] octanamide of a formula (I) shown in the description by using a salting and resolution method, and a method for separating N-[(1R,2R)-2-(2,3-dihydrogen-1,4-benzodioxyl-6-yl)-2-hydroxyl-1-(1-pyrrolidyl methyl) ethyl] octanamide from an enantiomer (RR,SS) N-[2-(2,3-dihydrogen-1,4-benzodialkyl-6-yl)-2-hydroxyl-1-(1-pyrrolidyl methyl) ethyl] octanamide) by taking a tartaric acid derivative or 4-hydroxyl dinaphtho[2,1-D:1',2'-F][1,3,2] diphosphepin-4-oxide and a derivative thereof, particularly D-(+)-di-p-methyl benzoyl tartaric acid and (-)-4-hydroxyl dinaphthyl [2,1-D:1',2'-F] [1,3,2] diphosphepin-4-oxide as a resolution agent through rotary resolution.

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