Regioselective protection at N-2 and derivatization at C-3 of indazoles

被引：60

作者：

Luo, Guanglin ^{[1
]}

Chen, Ling ^{[1
]}

Dubowchik, Gene ^{[1
]}

机构：

[1] Bristol Myers Squibb Pharmaceut Res Inst, Dept Neurosci Chem, Wallingford, CT 06443 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2006年 / 71卷 / 14期

关键词：

D O I：

10.1021/jo060607j

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Indazoles are regioselectively protected at N-2 by a 2-(tri-methylsilyl) ethoxymethyl (SEM) group using novel conditions. The SEM group can efficiently direct regioselective C-3 lithiation, and the resulting nucleophile can react with a wide range of electrophiles to generate novel indazole derivatives. The SEM group can be removed by treatment with TBAF in THF or aqueous HCl in EtOH.

引用

页码：5392 / 5395

页数：4

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