Stereoselective Synthesis of 尾-Lactam-triflones under Catalyst-Free Conditions

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• 作者：Zhongyan Huang ; Chen Wang ; Etsuko Tokunaga ; Yuji Sumii ; Norio Shibata
• 刊名：Organic Letters
• 出版年：2015
• 出版时间：November 20, 2015
• 年：2015
• 卷：17
• 期：22
• 页码：5610-5613
• 全文大小：391K
• ISSN：1523-7052

文摘

The first example of the synthesis of 尾-lactam-triflones is described. Treatment of 2-diazo-1-aryl-2-(trifluoromethylsulfonyl)ethanones 1c鈥?b>f with imines 2 under catalyst-free heating conditions provides pharmaceutically attractive multisubstituted 尾-lactam-triflones 3 in good to high yields with regio- and diastereoselectivities. A successive Wolff rearrangement and Staudinger [2 + 2] cycloaddition reaction are key elements for the success of this transformation.