Ru(II)-Catalyzed C-H Hydroxyalkylation and Mitsunobu Cyclization of N-Aryl Phthalazinones

被引:22
|
作者
Kim, Kunyoung [2 ]
Han, Sang Hoon [2 ]
Jeoung, Daeun [2 ]
Ghosh, Prithwish [2 ]
Kim, Saegun [2 ]
Kim, Seung Jun [2 ]
Ku, Jin-Mo [1 ]
Mishra, Neeraj Kumar [2 ]
Kim, In Su [2 ]
机构
[1] GBSA, Suwon, South Korea
[2] Sungkyunkwan Univ, Suwon, South Korea
来源
JOURNAL OF ORGANIC CHEMISTRY | 2020年 / 85卷 / 04期
基金
新加坡国家研究基金会;
关键词
DIRECT HYDROXYMETHYLATION; ANTITUMOR-ACTIVITY; BOND ACTIVATION; RU; ANNULATION; CINNOLINE; ALDEHYDES; ALKENES; DESIGN; DRUGS;
D O I
10.1021/acs.joc.9b03228
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Ruthenium (II)-catalyzed C (sp(2))-H functionalization of N-aryl phthalazinones with a range of aldehydes and activated ketone is described. Initial formation of hydroxyalkylated phthalazinones and subsequent Mitsunobu cyclization provided facile access to biologically relevant indazolophthalazinones. The utility of this method is highlighted by synthetic transformations into a series of potentially bioactive scaffolds.
引用
收藏
页码:2520 / 2531
页数:12
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