Late-stage diversification of biologically active pyridazinones via a direct C-H functionalization strategy

被引:6
作者
Li, Wei [1 ]
Fan, Zhoulong [2 ,3 ]
Geng, Kaijun [2 ,3 ]
Xu, Youjun [1 ]
Zhang, Ao [2 ,3 ]
机构
[1] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Shenyang 110016, Peoples R China
[2] Chinese Acad Sci, SIMM, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China
[3] Chinese Acad Sci, SIMM, SOMCL, Shanghai 201203, Peoples R China
关键词
CATALYZED DIRECT ARYLATION; STAPHYLOCOCCUS-AUREUS; MULTIKILOGRAM SYNTHESIS; COUPLING REACTIONS; INTERNAL ALKYNES; BOND FORMATION; ACTIVATION; OXIDATION; VERSATILE; ACCESS;
D O I
10.1039/c4ob02061h
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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.
引用
收藏
页码:539 / 548
页数:10
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