Late-stage diversification of biologically active pyridazinones via a direct C-H functionalization strategy.
Divergent C-H functionalization reactions (arylation, carboxylation, olefination, thiolation, acetoxylation, halogenation, naphthylation) using a pyridazinone moiety as an internal directing group were successfully established. This approach offers a late-stage, ortho-selective diversification of a biologically active pyridazinone scaffold. Seven series of novel pyridazinone analogues were synthesized conveniently as the synthetic precursors of potential sortase A (SrtA) inhibitors.
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China. xuyoujun@syphu.edu.cn.
Wei
W
Li
Zhoulong
Z
Fan
Kaijun
K
Geng
Youjun
Y
Xu
Ao
A
Zhang
D002244:Carbon / Q000737:chemistry*; D018360:Crystallography, X-Ray; D006859:Hydrogen / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D011724:Pyridazines / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization
D011724:Pyridazines; D002244:Carbon; D006859:Hydrogen