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Letters in Organic Chemistry

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ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

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Letter Article

Mild and Efficient Synthesis of Para-Substituted 2-Hydroxymethyl Piperazine

Author(s): Zijian Liang, Liyuan Guo, Qian Li, Chunyan Liu, Chao Liu and Shi Wu*

Volume 21, Issue 9, 2024

Published on: 20 February, 2024

Page: [737 - 743] Pages: 7

DOI: 10.2174/0115701786283816240123103232

Price: $65

Abstract

2-Hydroxymethyl piperazine is a crucial structural unit and essential intermediate in the drug development process. However, there are few reported methods for synthesizing 2- hydroxymethyl piperazine substituted at position 5. Herein, the 2-hydroxymethyl piperazines are synthesized from serine methyl ester hydrochloride and N-Boc-L-amino acids through a four-step reaction of condensation, deprotection, cyclisation, and reduction. This synthetic route has several advantages, including mild reaction conditions, availability of reagents, non-racemic composition, and the potential for gram-scale synthesis. In this study, we present a mild and effective synthetic method for preparing para-substituted 2-hydroxymethyl piperazine.

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