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Citation: Fang Jiaobing, Chen Yuchen, Cui Haonan, Wang Shiyu, Liu Mingzhe. Synthesis of trans-4-(Hydroxymethyl)piperidin-3-ol[J]. Chemistry, ;2019, 82(7): 663-665. shu

Synthesis of trans-4-(Hydroxymethyl)piperidin-3-ol

School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016

Corresponding author: Liu Mingzhe, mz_liu03@163.com
Received Date: 5 March 2019
Accepted Date: 12 April 2019

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Trans-4-(hydroxymethyl)piperidin-3-ol, a key intermediate of novel 5-hydroxytryptamine receptor agonist candidate, was synthesized by 4-hydroxymethylpyridin as starting material through four reaction steps including benzyl group protection, reduction with sodium borohydride, hydroboration-oxidation, deprotection of benzyl group. The total yield was up to 55.7%. The reaction products were characterized by IR, ¹H NMR and MS, and the synthetic process was also optimized.
- Trans-4-(hydroxymethyl)piperidin-3-ol,
- Hydroboration-oxidation,
- 5-Hydroxytryptamine receptor agonist,
- Benzyl protection
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