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Ru(II)-Catalyzed C-H Hydroxyalkylation and Mitsunobu Cyclization of N-Aryl Phthalazinones.
The Journal of Organic Chemistry ( IF 3.6 ) Pub Date : 2020-01-16 , DOI: 10.1021/acs.joc.9b03228
Kunyoung Kim 1 , Sang Hoon Han 1 , Daeun Jeoung 1 , Prithwish Ghosh 1 , Saegun Kim 1 , Seung Jun Kim 1 , Jin-Mo Ku 2 , Neeraj Kumar Mishra 1 , In Su Kim 1
Affiliation  

Ruthenium(II)-catalyzed C(sp2)-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.

中文翻译:

Ru(II)催化的N-芳基邻苯二氮杂苯环的CH羟烷基化和Mitsunobu环化。

描述了钌(II)催化的N-芳基酞嗪酮与一系列醛和活化的酮的C(sp2)-H官能化。羟烷基化酞嗪酮的最初形成和随后的Mitsunobu环化提供了与生物学相关的吲唑并邻苯二氮酮的便捷通道。通过合成转化为一系列可能具有生物活性的支架,突出了该方法的实用性。
更新日期:2020-01-17
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