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

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2015年 / 13卷 / 02期

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

页码：539 / 548

页数：10

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