A Concise Synthetic Method for Constructing 3-Substituted Piperazine-2-Acetic Acid Esters from 1,2-Diamines.

A Concise Synthetic Method for Constructing 3-Substituted Piperazine-2-Acetic Acid Esters from 1,2-Diamines.
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由1,2-二胺合成3-取代哌嗪-2-乙酸酯的简便方法。

DOI:
10.3390/molecules27113419
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发表时间:
2022-05-25
期刊:
Molecules (Basel, Switzerland)
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报道了一条合成2,3-取代哌嗪乙酸酯的短路线。光学纯的氨基酸可以高效地转化为1,2-二胺,可用于合成标题2,3-取代哌嗪,并具有较高的对映体纯度。新的路线首次促进了用其他方法难以实现的3-苯基取代-2-哌嗪乙酸酯的合成;然而,在这种情况下,产物进行了外消旋。
We report a short synthetic route for synthesizing 2,3-substituted piperazine acetic acid esters. Optically pure amino acids were efficiently converted into 1,2-diamines that could be utilized to deliver the title 2,3-substituted piperazines in five steps with a high enantiomeric purity. The novel route facilitated, for the first time, the synthesis of 3-phenyl substituted-2-piperazine acetic acid esters that were difficult to achieve using other methods; however, in this case, the products underwent racemization.
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