Affiliation:
1. School of Pharmacy, Hubei University of Science and Technology, Wuhan, China
2. Hubei Key Laboratory of Diabetes and Angiopathy, Hubei University of Science and Technology, Wuhan, China
Abstract
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.
Funder
Hubei University of Science and Technology, a Special Project on Diabetes and Angiopathy
Publisher
Bentham Science Publishers Ltd.