4.7 Article

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

期刊

JOURNAL OF ORGANIC CHEMISTRY
卷 85, 期 4, 页码 2520-2531

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.9b03228

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资金

  1. National Research Foundation of Korea (NRF) - Korea government (MSIP) [2017R1A2B2004786, 2017R1D1A1A09000574, 2018M3A9C8021792, 2019R1A4A2001451]
  2. National Research Foundation of Korea [2018M3A9C8021792, 2017R1A2B2004786, 2017R1D1A1A09000574, 2019R1A4A2001451] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)

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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.

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