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Updated: Jun 26, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
An alternative convenient synthesis of piperidazine-3-carboxylic acid derivatives
Mamoru Kaname1, Masae Yamada, Shigeyuki Yoshifuji
1Faculty of Pharmaceutical Sciences, Hokuriku University, Kanazawa, Japan.
Abstract:
The short-step synthesis of the unsubstituted, 5-hydroxy- and 5-chloropiperidazine-3-carboxylic acids using an aza Diels-Alder reaction between the 1,3-diene and azodicarboxylate was described. This synthetic methodology could be used for the preparation of the optically active piperazic acid in a 35% overall yield.
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