| 新型叶酸拮抗剂吡啶并嘌呤衍生物的环合反应研究 |
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| 引用本文： | 薛良敏,王锰,刘俊义,张志丽.新型叶酸拮抗剂吡啶并嘌呤衍生物的环合反应研究[J].化学通报,2018,81(7):653-656. |
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| 作者姓名： | 薛良敏 王锰 刘俊义 张志丽 |
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| 作者单位： | 北京大学医学部药学院;天然药物及仿生药物国家重点实验室 |
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| 摘 要： | 将6-取代-2,4-二氨基哌啶并3,2-d]嘧啶衍生物与N,N-二甲基甲酰胺、三氯乙酰氯在25℃反应2h,"一锅法"环合反应生成7-取代-2-氨基-7,8-二氢-6H-吡啶并1,2,3-gh]嘌呤衍生物,利用NMR、HRMS确定目标化合物的结构。考察了不同底物、反应底物比例、反应时间、温度对反应产率的影响,并提出可能的反应机理。该反应条件温和、效率高、操作简单。
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| 关 键 词： | N N-二甲基甲酰胺 三氯乙酰氯 环合反应 |
| 收稿时间： | 2018/3/19 0:00:00 |
| 修稿时间： | 2018/4/18 0:00:00 |
Cyclization Reaction of Pyridanopurine Derivatives as Novel Antifolate |
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| Xue Liangmin,Wang Meng,Liu Junyi and Zhang Zhili.Cyclization Reaction of Pyridanopurine Derivatives as Novel Antifolate[J].Chemistry,2018,81(7):653-656. |
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| Authors: | Xue Liangmin Wang Meng Liu Junyi and Zhang Zhili |
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| Institution: | School of Pharmaceutical Sciences,Peking University,Beijing,School of Pharmaceutical Sciences,Peking University,Beijing,State Key Laboratory of Natural and Biomimetic Drugs,School of Pharmaceutical Sciences,Peking University,Beijing,School of Pharmaceutical Sciences,Peking University,Beijing |
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| Abstract: | 7-Substituted 2-amine-8,9-dihydro-7H-pyrido1,2,3-gh]purin derivatives were synthesized by one-pot reaction with 6-substituted 2,4-diaminopyrido3,2-d]pyrimidine, DMF and trichloroacetyl chloride reacting at 25 oC for 2h. The effects of different substrate, reaction substrate ratio, reaction time and temperature on reaction yield were investigated. The structures of the target compounds were determined by NMR and MS, and the possible reaction mechanism was proposed. The reaction conditions are mild and easy to operate. |
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| Keywords: | DMF Trichloroacetyl chloride Cyclization reaction |
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