Mild and Efficient Synthesis of Para-Substituted 2-Hydroxymethyl Piperazine
LETTERS IN ORGANIC CHEMISTRY(2024)
摘要
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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关键词
2-Hydroxymethyl piperazine,synthesis,serine methyl ester,L-amino acids,non-racemic composition,gram-scale
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