Center for Drug Discovery, Department of Pathology and Immunology, Baylor College of Medicine, One Baylor Plaza, Houston, TX 77030, USA.
Department of Pharmacology and Chemical Biology, Baylor College of Medicine, One Baylor Plaza, Houston, TX 77030, USA.
Molecules. 2022 May 25;27(11):3419. doi: 10.3390/molecules27113419.
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.
我们报告了一种合成 2,3-取代哌嗪乙酸酯的短合成路线。光学纯氨基酸被高效地转化为 1,2-二胺，这些二胺可以在五步反应中以高对映体纯度得到标题 2,3-取代的哌嗪。该新路线首次促进了 3-苯基取代-2-哌嗪乙酸酯的合成，这是使用其他方法难以实现的；然而，在这种情况下，产物发生了外消旋化。
