Regioselective protection at N-2 and derivatization at C-3 of indazoles.
作者信息
Luo Guanglin, Chen Ling, Dubowchik Gene
机构信息
Department of Neurosciences Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06443, USA.
出版信息
J Org Chem. 2006 Jul 7;71(14):5392-5. doi: 10.1021/jo060607j.
PMID:16808535
Abstract
Indazoles are regioselectively protected at N-2 by a 2-(trimethylsilyl)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.
摘要
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