Rapid Access to 3-Aminoindazoles from Tertiary Amides

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• 作者：Patrick Cyr ; Sophie R茅gnier ; William S. Bechara ; Andr茅 B. Charette
• 刊名：Organic Letters
• 出版年：2015
• 出版时间：July 17, 2015
• 年：2015
• 卷：17
• 期：14
• 页码：3386-3389
• 全文大小：405K
• ISSN：1523-7052

文摘

A two-step synthesis of structurally diverse 3-aminoindazoles from readily available starting materials was developed. This sequence includes a one-pot synthesis of aminohydrazones through chemoselective Tfb>2b>O-mediated activation of tertiary amides and subsequent addition of nucleophilic hydrazides. These precursors then participate in an intramolecular ligand-free Pd-catalyzed C鈥揌 amination reaction. The azaheterocycles synthesized via this approach were further diversified through subsequent deprotection/functionalization reactions.