Synlett

Efficient and scalable synthesis of 3, 5, 7-trisubstituted 1H-indazoles as potent IKK2 inhibitors

X Lin, J Busch-Petersen, J Deng, C Edwards, Z Zhang…

文献索引：Lin, Xichen; Busch-Petersen, Jakob; Deng, Jianghe; Edwards, Christine; Zhang, Zhaoguo; Kerns, Jeffrey K. Synlett, 2008 , # 20 p. 3216 - 3220

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被引用次数: 5

摘要

Abstract Efficient and scalable chemical approaches to 3, 5, 7-trisubstituted 1H-indazoles were developed and applied to the synthesis of 1, 1-dimethylethyl 4-[7-(aminocarbonyl)-5- bromo-1H-indazol-3-yl]-1-piperidinecarboxylate, a key intermediate for 3, 5, 7-trisubstituted 1H-indazole, which was identified as a potent IKK2 inhibitor. The sequence allows for a scalable preparation of the target compound in eight steps and proceeds in 40% overall ...