RhIII-Catalyzed Redox-Neutral C-H Activation of Pyrazolones: An Economical Approach for the Synthesis of N-Substituted Indoles

被引：56

作者：

Fan, Zhoulong ^{[1
]}

Song, Shanshan ^{[2
]}

Li, Wei ^{[3
]}

Geng, Kaijun ^{[1
]}

Xu, Youjun ^{[3
]}

Miao, Ze-Hong ^{[2
]}

Zhang, Ao ^{[1
]}

机构：

[1] Chinese Acad Sci, SIMM, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China

[2] Chinese Acad Sci, SIMM, State Key Lab Drug Res, Shanghai 201203, Peoples R China

[3] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Shenyang 110016, Peoples R China

来源：

ORGANIC LETTERS | 2015年 / 17卷 / 02期

关键词：

OXIDIZING DIRECTING GROUP; INTERNAL ALKYNES; REGIOSELECTIVE SYNTHESIS; BOND FUNCTIONALIZATION; ISOQUINOLONE SYNTHESIS; OXIDATIVE ANNULATION; EFFICIENT SYNTHESIS; OXIME ESTERS; DERIVATIVES; OXIDANT;

D O I：

10.1021/ol503404p

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A new strategy is reported for the economical synthesis of indoles bearing an N-(3-aminobut-2-enoyl) substituent through RhIII-catalyzed redox-neutral C-H activation of pyrazolones and alkynes. This approach utilizes cheap substrates and mild reaction conditions to access a unique class of indoles via a N-N bond oxidative cleavage without loss of the N-terminus, therefore meeting all the atom/step/redox economy principles.

引用

页码：310 / 313

页数：4

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