| 从Baylis-Hillman加成物合成1，2，3，4-四氢苯并萘啶-2-酮衍生物 |
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| 引用本文： | 陈冬冬 徐静 杨春皓 谢毓元. 从Baylis-Hillman加成物合成1，2，3，4-四氢苯并萘啶-2-酮衍生物[J]. 中国化学, 2009, 27(4): 787-790. DOI: 10.1002/cjoc.200990131 |
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| 作者姓名： | 陈冬冬 徐静 杨春皓 谢毓元 |
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| 作者单位： | 中国科学院上海生命科学研究院上海药物研究所新药研究国家重点实验室,上海201203 |
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| 摘 要： | 本文介绍了（2）通过还原、两次环化的一锅串联反应制备了一系列1，2，3，4-四氢苯并萘啶-2-酮衍生物，反应条件温和，环境友好，产品易于分离，反应收率中等。起始原料可由Baylis－Hillman加成物通过Johnson-Claisen重排制备。
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| 关 键 词： | 1 2 3 4-四氢苯并萘啶酮 Baylis-Hillman反应 Johnson-Claisen重排 还原 双关环 |
| 收稿时间： | 2008-01-22 |
| 修稿时间： | 2008-11-03 |
Facile Synthesis of 1,2,3,4‐Tetrahydrobenzo[b][1,8]‐naphthyridin‐2‐one via Baylis‐Hillman Adducts |
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| Dongdong CHEN,Jing XU,Chunhao YANG,Yuyuan XIE. Facile Synthesis of 1,2,3,4‐Tetrahydrobenzo[b][1,8]‐naphthyridin‐2‐one via Baylis‐Hillman Adducts[J]. Chinese Journal of Chemistry, 2009, 27(4): 787-790. DOI: 10.1002/cjoc.200990131 |
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| Authors: | Dongdong CHEN Jing XU Chunhao YANG Yuyuan XIE |
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| Affiliation: | 1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, 555 Zu Chongzhi Road, Shanghai 201203, China;2. Tel.: 0086‐021‐50806600‐3512;3. Fax: 0086‐021‐50806770 |
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| Abstract: | Various benzo[b][1,8]naphthyridin‐2‐ones were synthesized by a one‐pot tandem reduction‐double cyclization from the corresponding (Z)‐ethyl 4‐cyano‐5‐(2‐nitrophenyl)‐pent‐4‐enoates, which were easily prepared via Johnson‐Claisen rearrangement from Baylis‐Hillman affixtures of 2‐nitrobenzaldehydes. The procedure has the advantages of easy handling and seperation under mild and green conditions, and the overall yields are moderate. |
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| Keywords: | benzo[b][1,8]naphthyridin‐2‐one Baylis‐Hillman reaction Johnson‐Claisen rearrangement reduction double cyclization |
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