| 邵钰,逯飞,刘小宇.不对称Heck反应合成手性哌啶衍生物[J].井冈山大学自然版,2024,45(1):23-26 |
| 不对称Heck反应合成手性哌啶衍生物 |
| syntheSIS OF chiral piperidine derivatives VIA ASYMMETRIC HECK REACTION |
| 投稿时间：2023-09-26 修订日期：2023-11-12 |
| DOI：10.3969/j.issn.1674-8085.2024.01.001 |
| 中文关键词: 不对称催化 Heck反应 手性哌啶衍生物 |
| 英文关键词: asymmetric catalysis Heck reaction chiral piperidine derivatives |
| 基金项目:国家自然科学基金项目(21871189)；四川省科技计划项目(2022JDJQ0048) |
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| 中文摘要: |
| 手性哌啶骨架广泛存在于药物和活性天然产物分子中。本研究发展了一种新型不对称Heck反应，用于合成手性哌啶衍生物。通过对反应条件进行筛选，得到了最优反应条件：催化剂为[Pd(allyl)Cl]2（5 mol %），配体为L5（10 mol %)，NaOMe（3.0 equiv）作碱，在110℃的混合溶剂（PhMe/MeOH = 5/1）中回流反应20 h。该不对称Heck反应显示出良好的底物普适性，可用于构建多种含有季碳中心的手性哌啶衍生物。 |
| 英文摘要: |
| Chiral piperidine backbones are widely found in the drugs and bioactive natural products. In the present study, a new asymmetric Heck reaction has been developed that allows synthesis of chiral piperidine derivatives. After screening of reaction conditions, the optimal conditions were obtained: [Pd(allyl)Cl]2 (5 mol %) as catalyst, L5 (10 mol%) as ligand, NaOMe (3.0 equiv) as base, mixed solvent (PhMe/MeOH = 5/1) at 110℃ for 20 hours. This method displays a good substrate scope, which could facilitate the preparation of chiral piperidine derivatives with quaternary stereogenic centers. |
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