Intramolecular Hydroamination of Difluoropropargyl Amides: Regioselective Synthesis of Fluorinated - and -Lactams

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• 作者：Santos Fustero ; Begoñ ; a Ferná ; ndez ; Paula Bello ; Carlos del Pozo ; Satoru Arimitsu ; Gerald B. Hammond
• 刊名：Organic Letters
• 出版年：2007
• 出版时间：October 11, 2007
• 年：2007
• 卷：9
• 期：21
• 页码：4251 - 4253
• 全文大小：66K
• 年卷期：v.9,no.21(October 11, 2007)
• ISSN：1523-7052

文摘

Functionalized gem-difluoro - and -lactams were synthesized through a novel intramolecular hydroamination reaction of difluoropropargylamides. -Lactams were obtained via a Baldwin disfavored 4-exo-digonal cyclization using palladium acetate as the catalyst, whereas -lactamswere produced under basic conditions. Acid hydration of -lactams produced ketoamides or hemiaminals selectively.