| 方教冰,陈雨辰,崔浩楠,王诗宇,刘明哲.化学通报,2019,82(7):663-665. |
| 反-4-羟甲基哌啶-3-醇的合成 |
| Synthesis of trans-4-(Hydroxymethyl)piperidin-3-ol |
| 投稿时间：2019-03-05 修订日期：2019-04-10 |
| DOI： |
| 中文关键词: 反-4-羟甲基哌啶-3-醇 硼氢化氧化 5-羟色胺受体激动剂 苄基保护 |
| 英文关键词:Trans-4-(hydroxymethyl)piperidin-3-ol, Hydroboration-oxidation, 5-Hydroxytryptamine receptor agonist, Benzyl protection |
| 基金项目:国家自然科学基金（21875145），辽宁省自然科学基金（20180550392） |
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| 中文摘要: |
| 以4-羟甲基吡啶为原料，经苄基保护，硼氢化钠还原，硼氢化氧化和脱苄基保护等四步反应得到新型5-羟色胺受体激动剂的关键中间体，反-4-羟甲基哌啶-3-醇。总收率达55.7%。产物结构经IR、1H NMR和MS分析确证，并对合成工艺进行了优化。 |
| 英文摘要: |
| Trans-4-(hydroxymethyl)piperidin-3-ol, a key intermediate of novel 5-hydroxytryptamine receptor agonist candidate, was synthesized by 4-hydroxymethyl pyridine 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. |
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