An Approach for the Synthesis of Pyrazolo[1,5-a]pyrimidines via Cu(II)-Catalyzed [3+3] Annulation of Saturated Ketones with Aminopyrazoles
文献类型：期刊论文
| 作者 | Ren,Jian; Ding,Shihua; Li,Xiaonian; Bi,Ran; Zhao,Qinshi
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| 刊名 | JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2021 |
| 卷号 | 86期号:18页码:12762-12771 |
| 关键词 | BIOLOGICAL EVALUATION REGIOSELECTIVE SYNTHESIS CASCADE REACTIONS FUNCTIONALIZATION DEHYDROGENATION DISCOVERY POTENT BOND SAR |
| ISSN号 | 0022-3263 |
| DOI | 10.1021/acs.joc.1c01343 |
| 英文摘要 | A one-step synthesis of diversely substituted pyrazolo[1,5-a]pyrimidines from saturated ketones and 3-aminopyrazoles is presented. This transformation involves the in situ formation of alpha,beta-unsaturated ketones via a radical process, followed by [3+3] annulation with 3-aminopyrazoles in one pot. Mechanistic studies have shown that the dual C(sp(3))-H bond functionalization of inactive ketones is required for the formation of the title compounds. Notably, this dehydrogenative coupling process provides access to a host of functionalized pyrazolo[1,5-a]pyrimidines with antitumor potential from commercially available substrates. |
| WOS记录号 | WOS:000697353500027 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/73013]  |
| 专题 | 中国科学院昆明植物研究所 |
| 作者单位 | 1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China 2.Chinese Acad Sci, Kunming Inst Bot, Yunnan Key Lab Nat Med Chem, Kunming 650201, Yunnan, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ren,Jian,Ding,Shihua,Li,Xiaonian,et al. An Approach for the Synthesis of Pyrazolo[1,5-a]pyrimidines via Cu(II)-Catalyzed [3+3] Annulation of Saturated Ketones with Aminopyrazoles[J]. JOURNAL OF ORGANIC CHEMISTRY,2021,86(18):12762-12771. |
| APA | Ren,Jian,Ding,Shihua,Li,Xiaonian,Bi,Ran,&Zhao,Qinshi.(2021).An Approach for the Synthesis of Pyrazolo[1,5-a]pyrimidines via Cu(II)-Catalyzed [3+3] Annulation of Saturated Ketones with Aminopyrazoles.JOURNAL OF ORGANIC CHEMISTRY,86(18),12762-12771. |
| MLA | Ren,Jian,et al."An Approach for the Synthesis of Pyrazolo[1,5-a]pyrimidines via Cu(II)-Catalyzed [3+3] Annulation of Saturated Ketones with Aminopyrazoles".JOURNAL OF ORGANIC CHEMISTRY 86.18(2021):12762-12771. |
入库方式： OAI收割
来源：昆明植物研究所
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