| 薛良敏,王锰,刘俊义,张志丽.化学通报,2018,81(7):653-656. |
| 新型叶酸拮抗剂吡啶并嘌呤衍生物的环合反应研究 |
| Cyclization Reaction of Pyridanopurine Derivatives as Novel Antifolate |
| 投稿时间：2018-03-19 修订日期：2018-04-18 |
| DOI： |
| 中文关键词: N,N-二甲基甲酰胺 三氯乙酰氯 环合反应 |
| 英文关键词:DMF, Trichloroacetyl chloride, Cyclization reaction |
| 基金项目: |
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| 摘要点击次数: 1645 |
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| 中文摘要: |
| 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25oC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。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。利用NMR、MS确定目标化合物结构,并提出该反应可能的反应机理。该反应条件温和、效率高、操作简单。 |
| 英文摘要: |
| 7-Substituted 2-amine-8,9-dihydro-7H-pyrido[1,2,3-gh]purin derivatives were synthesized by one-pot reaction with 6-substituted 2,4-diaminopyrido[3,2-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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