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Updated: Jul 11, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
A practical synthesis of differentially protected 2-(hydroxymethyl)piperazines
1Pfizer Global Research and Development, 34790 Ardentech Court, Fremont, California 94555, USA.
Abstract:
An efficient and scalable synthesis of three differentially protected 2-(hydroxymethyl)piperazines is presented, starting from optically active and commercially available (2S)-piperazine-2-carboxylic acid dihydrochloride. These synthetic building blocks are useful in the preparation of biologically active compounds and as chemical scaffolds for the construction of combinatorial libraries.
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