首页> 外国专利> Process for preparing optically active N-tert-butyl-2-piperazinecarboxamide and its racemization process (PROCESS FOR PRODUCING OPTICALLY ACTIVE N-TERT-BUTYL-2-PIPERAZINECARBOXAMIDE AND METHOD OF RACEMIZING THE AMIDE)

Process for preparing optically active N-tert-butyl-2-piperazinecarboxamide and its racemization process (PROCESS FOR PRODUCING OPTICALLY ACTIVE N-TERT-BUTYL-2-PIPERAZINECARBOXAMIDE AND METHOD OF RACEMIZING THE AMIDE)

机译:光学活性的N-叔丁基-2-哌嗪甲酰胺的制备方法及其外消旋过程(制备光学活性的N-叔丁基-2-哌嗪羧酰胺的方法及将其芳构化的方法)

摘要

(R, S)-N-tert-butyl-2-piperazinecarboxamide was subjected to optical resolution using optically active lactic acid, optically active malic acid or optically active tartaric acid as a resolving agent to obtain optically active N-tert-Razine carboxyamide. Optically active N-tert-butyl-2-piperazinecarboxamide which is useful as a medicament intermediate or the like is obtained with high optical purity. Further, by optically cleaving the optically active N-tert-butyl-2-piperazinecarboxamide in the presence of a basic compound and performing optical resolution, an enantiomer which has remained as an unavailable enantiomer by the above optical resolution can be usefully used.
机译:使用旋光性乳酸,旋光性苹果酸或旋光性酒石酸作为拆分剂对(R,S)-N-叔丁基-2-哌嗪甲酰胺进行旋光拆分,从而获得旋光性N-叔-雷嗪羧酰胺。获得具有高光学纯度的旋光性N-叔丁基-2-哌嗪甲酰胺,其用作药物中间体等。另外,通过在碱性化合物的存在下将光学活性的N-叔丁基-2-哌嗪甲酰胺光学裂解并进行旋光拆分,可以有效地使用通过上述旋光拆分而不能得到的对映异构体。

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