首页> 外国专利> Process for preparing extreme optically pure 2-({(5S)-2-oxo-3-4-(3-oxo-4-morpholinyl)phenyl-1,3oxazolidin-5-yl}methyl)-1H-isoindole-1,3(2H)-dione

Process for preparing extreme optically pure 2-({(5S)-2-oxo-3-4-(3-oxo-4-morpholinyl)phenyl-1,3oxazolidin-5-yl}methyl)-1H-isoindole-1,3(2H)-dione

机译:制备极端光学纯的2-({((5S)-2-oxo-3- [4-(3-oxo-4-吗啉基)苯基] -1,3-恶唑烷丁-5-基}甲基)-1H-异吲哚- 1,3(2H)-二酮

摘要

The present invention relates to a process for preparing optically highly pure compound of formula I, reacting 2 - ((2R) -2-hydroxy-3- [4- (3-oxo-4-morpholinyl) phenyl] aminopropyl) -1H-isoindole-1,3 (2H) -dione, the compound of formula III, containing (2S) -isomer, compound of formula IIIb with N, N-carbonyldiimidazole in tetrahydrofuran in the absence of the catalyst 4-dimethylaminopyridine, the reaction being carried out such that it is terminated when the reaction mixture still contains unreacted material III at which is between 3 and 5 times the original volume (2S) -isomer in a feed substance III.
机译:本发明涉及一种使2-((2R)-2-羟基-3- [4-(3-氧代-4-吗啉基)苯基]氨基丙基)-1H-反应的光学高度纯的式I化合物的制备方法。异吲哚-1,3(2H)-二酮,式(Ⅲ)化合物,含(2S)-异构体,式(Ⅲb)化合物与N,N-羰基二咪唑在四氢呋喃中,在催化剂4-二甲基氨基吡啶不存在的情况下进行当反应混合物中仍含有未反应的原料Ⅲ时,它就终止了,该原料的量是原料Ⅲ中原始体积(2S)-异构体的3-5倍。

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