Asymmetric Synthesis of CF3- and Indole-Containing Thiochromanes via a Squaramide-Catalyzed Michael–Aldol Reaction

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• 作者：Yuanyuan Zhu ; Zhenghao Dong ; Xin Cheng ; Xiaoling Zhong ; Xiaolin Liu ; Li Lin ; Zhiqiang Shen ; Peiju Yang ; Yuan Li ; Hailin Wang ; Wenjin Yan ; Kairong Wang ; Rui Wang
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：August 5, 2016
• 年：2016
• 卷：18
• 期：15
• 页码：3546-3549
• 全文大小：397K
• 年卷期：0
• ISSN：1523-7052

文摘

A Michael–aldol reaction of 2-mercaptobenzaldehyde with β-indole-β-CF₃ enones catalyzed by a squaramide has been realized. The method affords a series of 2-CF₃-2-indole-substituted thiochromanes featuring a CF₃-containing quaternary stereocenter in excellent yields, diastereoselectivities, and enantioselectivities.