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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对位取代 2-羟甲基哌嗪的温和高效合成

2-羟甲基哌嗪是药物开发过程中重要的结构单元和必需的中间体。然而，目前5位取代的2-羟甲基哌嗪的合成方法报道较少。本文以丝氨酸甲酯盐酸盐与N-Boc-L-氨基酸为原料，经过四步缩合反应合成2-羟甲基哌嗪。脱保护、环化和还原。该合成路线具有多种优点，包括反应条件温和、试剂的可用性、非外消旋组成以及克级合成的潜力。在本研究中，我们提出了一种温和有效的合成方法来制备对位取代的2-羟甲基哌嗪。