Stereoselective synthesis of enantiopure N-protected-3-arylpiperazines from keto-esters
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- 作者：Mouhamad Jida ; Guillaume Laconde ; Olivier-Mohamad Soueidan ; Nicolas Lebegue ; Germain Revelant ; Lydie Pelinski ; Francine Agbossou-Niedercorn ; Benoit Deprez ; Rebecca Deprez-Poulain
- 关键词：Stereoselective ring opening ; Cyclocondensation ; Lactams ; Piperazines ; Nitrogen heterocycles ; Chiral
- 刊名：Tetrahedron Letters
- 出版年：2012
- 出版时间：26 September, 2012
- 年：2012
- 卷：53
- 期：39
- 页码：5215-5218
- 全文大小：677 K
文摘
An efficient method for a stereoselective synthesis of optically pure N-Boc-3-arylpiperazines has been developed. After optimization of the protecting group strategy and experimental conditions, compounds were obtained via a highly stereoselective synthesis in up to 45 % overall yield. This is a practical route to optically pure piperazines for medicinal chemistry.